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Results for "

inhibitor

" in MCE Product Catalog:

9866

Inhibitors & Agonists

46

Screening Libraries

22

Dye Reagents

18

Biochemical Assay Reagents

256

Peptides

15

MCE Kits

47

Inhibitory Antibodies

1022

Natural
Products

133

Recombinant Proteins

483

Isotope-Labeled Compounds

Targets Recommended: PAI-1 SNIPERs
Cat. No. Product Name Target Research Areas
  • HY-16695
    MIM1

    inhibitor of Mcl-1

    Bcl-2 Family Cancer
    MIM-1 is an inhibitor of myeloid cell factor 1 (Mcl-1).
  • HY-131005
    Eph inhibitor 2

    Ephrin Receptor Cancer
    Eph inhibitor 2 (Example 35) is a Eph family tyrosine kinase inhibitor.
  • HY-146709
    BET bromodomain inhibitor 2

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC50 of 14.1 µM.
  • HY-145826
    Mcl-1 inhibitor 8

    Bcl-2 Family Cancer
    Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112.
  • HY-142934
    RORγt inhibitor 2

    ROR Inflammation/Immunology Cancer
    RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC50 of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt.
  • HY-142853
    Carbonic anhydrase inhibitor 3

    Carbonic Anhydrase Endocrinology
    Carbonic anhydrase inhibitor 3 (compound 11g) is a carbonic anhydrase II inhibitor. Carbonic anhydrase inhibitor 3 reduces the intraocular pressure in glaucomatous rabbits.
  • HY-142849
    Carbonic anhydrase inhibitor 2

    Carbonic Anhydrase Endocrinology
    Carbonic anhydrase inhibitor 3 (compound 7c) is a carbonic anhydrase II inhibitor. Carbonic anhydrase inhibitor 3 reduces the intraocular pressure in glaucomatous rabbits.
  • HY-142460
    KRAS G12C inhibitor 28

    Ras Cancer
    KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1).
  • HY-115880
    KRAS G12D inhibitor 3

    Ras Cancer
    KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146).
  • HY-142458
    KRAS G12C inhibitor 27

    Ras Cancer
    KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737).
  • HY-142457
    KRAS G12C inhibitor 26

    Ras Cancer
    KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737).
  • HY-115880A
    KRAS G12D inhibitor 3 TFA

    Ras Cancer
    KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146).
  • HY-119374
    BRM/BRG1 ATP Inhibitor-1

    Epigenetic Reader Domain Cancer
    BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.
  • HY-118933
    Calpain Inhibitor VI

    SJA6017

    Proteasome Others
    Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.
  • HY-146739
    BRD4 Inhibitor-19

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-19 is BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research.
  • HY-147705
    PPARγ phosphorylation inhibitor 1

    PPAR Metabolic Disease
    PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects.
  • HY-115999
    Carbonic anhydrase inhibitor 12

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.
  • HY-112412
    PDGFR Tyrosine Kinase Inhibitor III

    PDGF Receptor Tyrosine Kinase inhibitor III

    PDGFR Neurological Disease
    PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis.
  • HY-142467
    HIV-1 inhibitor-11

    HIV Infection
    HIV-1 inhibitor-11, a fused pyridine ring derivative, is a HIV-1 inhibitor. WO2021104413A1 ( compound 1-1b).
  • HY-143280
    Topoisomerase II inhibitor 4

    Topoisomerase Cancer
    Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
  • HY-10096
    GSK-3β inhibitor 9

    GSK-3 Neurological Disease
    GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. GSK-3β inhibitor 9 shows good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 can be used for the research of Alzheimer’s disease.
  • HY-149018
    ATX inhibitor 22

    Phosphodiesterase (PDE) Cancer
    ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) with IC50 of 218 nM but lost its inhibitory activity of LPAR1.
  • HY-143402
    Topoisomerase I/II inhibitor 2

    Topoisomerase Cancer
    Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in treating liver cancer.
  • HY-143235
    BRD4 Inhibitor-15

    Epigenetic Reader Domain Apoptosis Bcl-2 Family Caspase c-Myc Cancer
    BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research.
  • HY-143721
    SSAO inhibitor-2

    Monoamine Oxidase Metabolic Disease Cardiovascular Disease Inflammation/Immunology
    SSAO inhibitor-2 (Compound 1) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 10-100 μM for human SSAO and MAO-A, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
  • HY-143723
    SSAO inhibitor-3

    Monoamine Oxidase Metabolic Disease Cardiovascular Disease Inflammation/Immunology
    SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
  • HY-70005
    CPA inhibitor

    Carboxypeptidase inhibitor

    Carboxypeptidase Metabolic Disease
    CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a Ki of 0.32 μM.
  • HY-136123
    Tubulin inhibitor 8

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
  • HY-136122
    Tubulin inhibitor 7

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
  • HY-136121
    Tubulin inhibitor 6

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
  • HY-147891
    Angiogenesis inhibitor 3

    Apoptosis Cancer
    Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos.
  • HY-147890
    Angiogenesis inhibitor 2

    Apoptosis Cancer
    Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos.
  • HY-146711
    Tubulin inhibitor 24

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity.
  • HY-145821
    Tubulin inhibitor 15

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells.
  • HY-145822
    Tubulin inhibitor 16

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells.
  • HY-115956
    Tubulin inhibitor 18

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases.
  • HY-144818
    Tubulin inhibitor 23

    Apoptosis Microtubule/Tubulin Cancer
    Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia.
  • HY-115957
    Tubulin inhibitor 19

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 19 (compound 9b) is a potent inhibitor of tubulin. Tubulin inhibitor 19 is an indole chalcone compound. Tubulin inhibitor 19 has the potential for the research of cancer diseases.
  • HY-145828
    Microtubule inhibitor 2

    Microtubule/Tubulin Ferroptosis Cancer
    Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
  • HY-115958
    Tubulin inhibitor 20

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 20 (compound 1) is a potent inhibitor of tubulin. Tubulin inhibitor 20 has the potential for the research of cancer diseases.
  • HY-147888
    Tubulin inhibitor 29

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site.
  • HY-144766
    ATX inhibitor 13

    Apoptosis Others Cancer
    ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation.
  • HY-128617
    Legumain inhibitor 1

    Others Cancer
    Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
  • HY-143420
    ATX inhibitor 15

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model.
  • HY-145820
    Tubulin inhibitor 14

    Apoptosis Thrombin Microtubule/Tubulin Cancer
    Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features.
  • HY-143251
    Tubulin inhibitor 13

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 13 (E27) is a potent tubulin inhibitor with an IC50 value of 16.1 μM for the tubulin polymerization inhibition. Tubulin inhibitor 13 inhibits migration and invasion of cancer cells, induces apoptosis and has anticancer activity.
  • HY-112607
    Tubulin inhibitor 1

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
  • HY-142644
    ATX inhibitor 7

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.
  • HY-147726
    Microtubule inhibitor 5

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability.
  • HY-132196
    BTK inhibitor 18

    Btk Inflammation/Immunology
    BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.
  • HY-146672
    ITK inhibitor 6

    Itk Cancer
    ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.
  • HY-147727
    Microtubule inhibitor 6

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization.
  • HY-13276
    IRAK inhibitor 2

    IRAK Inflammation/Immunology
    IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .
  • HY-131705
    BTK inhibitor 17

    Btk Inflammation/Immunology
    BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
  • HY-10217
    Thrombin Inhibitor 2

    Thrombin Cardiovascular Disease
    Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity.
  • HY-144817
    Tubulin inhibitor 27

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 27 (DYT-1) is a tubulin polymerisation inhibitor with an IC50 of 25.6 µM. Tubulin inhibitor 27 shows anti-angiogenesis and antitumor activities.
  • HY-146889
    ATX inhibitor 16

    Others Cancer
    ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 µM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells.
  • HY-146890
    ATX inhibitor 17

    Others Cancer
    ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 µM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells.
  • HY-139881
    BTK inhibitor 19

    Btk Cancer
    BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
  • HY-143730
    BTK inhibitor 20

    Btk Cancer
    BTK inhibitor 20 is a potent BTK inhibitor with an IC50 of 8 nM.
  • HY-142296
    RORγt inhibitor 1

    ROR Inflammation/Immunology
    RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC50 value of 1 nM.
  • HY-144748
    Tubulin inhibitor 17

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 17 (Compound 3b) is a tubulin polymerization inhibitor with an IC50 of 12.38 µM. Tubulin inhibitor 17 has anticancer activities and induces cell apoptosis.
  • HY-15358
    ALK inhibitor 2

    Anaplastic lymphoma kinase (ALK) FAK Cancer
    ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
  • HY-15357
    ALK inhibitor 1

    Anaplastic lymphoma kinase (ALK) FAK Cancer
    ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
  • HY-146778
    Tubulin inhibitor 25

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis.
  • HY-146366
    Tubulin inhibitor 26

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight.
  • HY-143250
    Tubulin inhibitor 12

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity.
  • HY-W013478
    PTP inhibitor 1

    Phosphatase Cancer
    PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect.
  • HY-112913
    SOCE inhibitor 1

    CRAC Channel Metabolic Disease Neurological Disease
    SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM.
  • HY-125997
    BTK inhibitor 10

    Btk Inflammation/Immunology
    BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
  • HY-148037
    Thrombin inhibitor 5

    Proteasome Cardiovascular Disease
    Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism.
  • HY-147887
    Tubulin inhibitor 28

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells.
  • HY-146122
    ATX inhibitor 19

    Phosphodiesterase (PDE) Cancer
    ATX inhibitor 19 (compound 22) is a potent ATX (autotaxin) inhibitor, with an IC50 of 156 nM.
  • HY-146124
    ATX inhibitor 21

    Phosphodiesterase (PDE) Cancer
    ATX inhibitor 21 (compound 8) is a potent ATX (autotaxin) inhibitor, with an IC50 of 3490 nM.
  • HY-143419
    ATX inhibitor 14

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 14 (compound 4), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 0.41 nM. ATX inhibitor 14 has the potential for fibrosis relevant diseases research.
  • HY-147725
    Microtubule inhibitor 4

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization.
  • HY-143237
    ATX inhibitor 11

    Phosphodiesterase (PDE) Others
    ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research.
  • HY-10439
    HPGDS inhibitor 1

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
  • HY-144647
    SP inhibitor 1

    SARS-CoV Virus Protease Infection
    SP inhibitor 1 (compound 34) is a selective SARS-CoV-2 spike protein (SP) inhibitor with an IC50 of 3.26 μM, >25 μM, >25 μM for SP, M pro and PL pro protein, respectively. SP inhibitor 1 is a vitro SARS-CoV-2 replication inhibitor at non-toxic concentrations (0.3250<5.98 μM). SP inhibitor 1 shows cellular antiviral activity.
  • HY-124793A
    GAK inhibitor 49 hydrochloride

    Others Infection
    GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.
  • HY-124793
    GAK inhibitor 49

    Others Infection
    GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
  • HY-U00377
    Cathepsin Inhibitor 2

    Cathepsin Cancer Inflammation/Immunology
    Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.
  • HY-146123
    ATX inhibitor 20

    Phosphodiesterase (PDE) Cancer
    ATX inhibitor 20 (compound 24) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.3 nM.
  • HY-119938
    Tuberculosis inhibitor 1

    Bacterial Infection
    Tuberculosis inhibitor 1 is a potent and non-cytotoxic trypanosoma brucei growth inhibitor with an EC50 of 5 nM.
  • HY-143581
    ATX inhibitor 8

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 8 is a Autotaxin (ATX) inhibitor extracted from patent WO2018212534A1 compound 96.
  • HY-13278
    IRAK inhibitor 4

    IRAK Inflammation/Immunology
    IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
  • HY-15775
    Arginase inhibitor 1

    Arginase Cancer
    Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
  • HY-13278A
    IRAK inhibitor 4 trans

    IRAK Inflammation/Immunology
    IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.
  • HY-143583
    ATX inhibitor 10

    Others Cancer Neurological Disease
    ATX inhibitor 10 is a potent inhibitor of ATX. ATX inhibitor 10 is s nitrogen-containing heterocyclic compound. ATX plays a role in causing pathological conditions including fibrosis, arthritis, neurodegeneration, neuropathic pain, and cancer. ATX inhibitor 10 has the potential for the research of ATX related diseases (extracted from patent WO2021115375A1, compound 35).
  • HY-132884
    TTK inhibitor 3

    Others Cancer
    TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
  • HY-111506
    Aurora inhibitor 1

    Aurora Kinase Cancer
    Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively.
  • HY-13280
    IRAK inhibitor 6

    IRAK Inflammation/Immunology
    IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC50 of 160 nM.
  • HY-18928
    FAK inhibitor 5

    FAK Cancer
    FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
  • HY-109574
    Raf inhibitor 2

    Raf Cancer
    Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.
  • HY-133019
    ATX inhibitor 5

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.
  • HY-101053
    Src Inhibitor 1

    Src Kinase inhibitor 1; Src-l1

    Src Cancer
    Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
  • HY-144797
    Tubulin inhibitor 22

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction.
  • HY-146662
    HPGDS inhibitor 3

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
  • HY-111489
    LMPTP inhibitor 1

    Phosphatase Metabolic Disease
    LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  • HY-U00370
    Thrombin inhibitor 1

    Thrombin Cardiovascular Disease
    Thrombin inhibitor 1 is a potent thrombin inhibitor (Ki=0.66 nM, 2xaPTT=0.43 μM).
  • HY-111489A
    LMPTP inhibitor 1 hydrochloride

    Phosphatase Metabolic Disease
    LMPTP inhibitor 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  • HY-111489B
    LMPTP inhibitor 1 dihydrochloride

    Phosphatase Metabolic Disease
    LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  • HY-147761
    GAK inhibitor 2

    Others Infection
    GAK inhibitor 2 (Compound 14g) is a potent cyclin G-associated kinase (GAK) inhibitor with an IC50 of 0.024 μM. GAK inhibitor 2 shows antiviral activity with an EC50 of 1.049 μM against dengue virus (DENV).
  • HY-130255
    BTK inhibitor 13

    Btk Inflammation/Immunology
    BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM.
  • HY-111410
    ATX inhibitor 1

    Phosphodiesterase (PDE) Cancer
    ATX inhibitor 1 is a potent ATX (IC50=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
  • HY-146387
    SIRT5 inhibitor 3

    Sirtuin Cancer Neurological Disease
    SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases.
  • HY-144743
    ATX inhibitor 12

    Phosphodiesterase (PDE) Others
    ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research.
  • HY-143582
    ATX inhibitor 9

    Others Cancer
    ATX inhibitor 9 is a potent inhibitor of ATX. ATX inhibitor 9 is a thickened heteroaryl derivatives compound. Autotaxin (ATX), also known as ENPP2, is a secreted enzyme that is highly expressed mainly in cancer cells, bronchial epithelial cells and alveolar macrophages in the lung. ATX inhibitor 9 has the potential for the research of cancer or fibrous degenerative disease (extracted from patent WO2021078227A1, compound 3).
  • HY-128580
    FAK inhibitor 2

    FAK Cancer
    FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50  of 0.07 nM, with antitumor and anti-angiogenesis activities.
  • HY-126134
    HPGDS inhibitor 2

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.
  • HY-112712
    Cyclophilin inhibitor 1

    HCV Infection
    Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a.
  • HY-146671
    ITK inhibitor 5

    Itk Cancer
    ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC50s of 5.6, 25 nM for ITK, BTK, respectively.
  • HY-146648
    Cyclophilin inhibitor 3

    HCV Infection
    Cyclophilin inhibitor 3 (compound 7c) is a potent cyclophilin A (CypA) inhibitor with an potent anti-HCV activity (EC50 of 4.2 μM).
  • HY-111451
    ATR inhibitor 1

    ATM/ATR Cancer
    ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 µΜ.
  • HY-114317
    MARK4 inhibitor 1

    AMPK Apoptosis Cancer
    MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
  • HY-115970
    Tubulin inhibitor 21

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 21 (compound 6f), a chalcone- and melatonin- based hybrid, is a potent tubulin inhibitor. Tubulin inhibitor 21 induces a remarkable cytotoxic activity toward SW480 cells (IC50=0.26 μM) with lower effect against nonmalignant cells.
  • HY-144774
    Topoisomerase I inhibitor 5

    Topoisomerase DNA/RNA Synthesis Apoptosis Cancer
    Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
  • HY-144366
    P-gp inhibitor 3

    P-glycoprotein Cancer
    P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
  • HY-13973A
    GSK-3 inhibitor 1

    GSK-3 Metabolic Disease
    GSK-3 inhibitor 1 is an inhibitor of GSK-3.
  • HY-146348
    Tuberculosis inhibitor 5

    Bacterial Infection
    Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent.
  • HY-143715
    Cereblon inhibitor 1

    Ligands for E3 Ligase Cancer
    Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research.
  • HY-126328
    PKC-theta inhibitor 1

    PKC Inflammation/Immunology
    PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.
  • HY-150983
    ATP synthase inhibitor 2

    ATP Synthase Infection
    ATP synthase inhibitor 2 is a Pseudomonas aeruginosa (PA) ATP synthase inhibitor (IC50=10 μg/mL). ATP synthase inhibitor 2 can inhibit Pseudomonas aeruginosa (PA) ATP synthesis activity completely at 128 μg/mL.
  • HY-143461
    CK2 inhibitor 3

    Casein Kinase Cancer
    CK2 inhibitor 3 is a potent CK2 inhibitor with IC50 value of 280 nM. CK2 inhibitor 3 inhibits endocellular CK2, significantly affects viability of tumour cells and shows remarkable selectivity on a panel of 320 kinases.
  • HY-146064
    OPN expression inhibitor 1

    Others Cancer
    OPN expression inhibitor 1 (Compound 11) is an osteopontin (OPN) expression inhibitor. OPN expression inhibitor 1 can be used for breast cancer research.
  • HY-151421
    Chitin synthase inhibitor 11

    Fungal Cancer Infection
    Chitin synthase inhibitor 11 is a chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 11 shows excellent CHS inhibitory activity with an IC50 value of 0.10 mM. Chitin synthase inhibitor 11 has broad-spectrum antifungal activity in vitro. Chitin synthase inhibitor 11 can be used for the research of invasive fungal infections (IFIs).
  • HY-143265
    Topoisomerase I inhibitor 2

    Topoisomerase Apoptosis Caspase Cancer
    Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
  • HY-151432
    URAT1 inhibitor 3

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.
  • HY-107662
    TCS PrP Inhibitor 13

    Apoptosis Cancer Infection
    TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrP C) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis.
  • HY-146497
    Topoisomerase I inhibitor 7

    Topoisomerase Cancer
    Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor drug candidates among the heteroarene-fused anthraquinones.
  • HY-128726
    ITK inhibitor 2

    Itk Inflammation/Immunology
    ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM.
  • HY-12860
    Notch inhibitor 1

    Notch Cancer
    Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer.
  • HY-14177
    Raf inhibitor 1

    Raf Cancer
    Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
  • HY-147710
    PIN1 inhibitor 2

    MicroRNA Cancer
    PIN1 inhibitor 2 (compound 12) is a potent PIN1 inhibitor. PIN1 inhibitor 2 shows antitumor activity with an IC50 of 9.55 µM for MCF7 cells. PIN1 inhibitor 2 has the potential for the research of breast cancer.
  • HY-141659
    USP30 inhibitor 18

    Deubiquitinase Cancer
    USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy.
  • HY-151418
    Chitin synthase inhibitor 8

    Fungal Infection
    Chitin synthase inhibitor 8 is a chitin synthase (CHS) inhibitor with broad-spectrum antifungal activity. Chitin synthase inhibitor 8 can be used in the research of fungi infection.
  • HY-151419
    Chitin synthase inhibitor 9

    Fungal Infection
    Chitin synthase inhibitor 9 is a chitin synthase (CHS) inhibitor with broad-spectrum antifungal activity. Chitin synthase inhibitor 9 can be used in the research of fungi infection.
  • HY-112270
    Glutaminyl Cyclase Inhibitor 2

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM.
  • HY-144375
    Monoacylglycerol lipase inhibitor 1

    MAGL Others
    Monoacylglycerol lipase inhibitor 1 is a potent monoacylglycerol lipase inhibitor (compound 13).
  • HY-U00319
    Lipid peroxidation inhibitor 1

    Others Neurological Disease
    Lipid peroxidation inhibitor 1 is a lipid peroxidation inhibitor with an IC50 of 0.07 μM.
  • HY-112269
    Glutaminyl Cyclase Inhibitor 1

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM.
  • HY-144452
    Immunoproteasome inhibitor 1

    Proteasome Cancer
    Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the treatment of certain neoplastic diseases.
  • HY-143301
    Topoisomerase I inhibitor 4

    Topoisomerase Cancer
    Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer.
  • HY-14177A
    Raf inhibitor 1 dihydrochloride

    Raf Cancer
    B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
  • HY-150686
    Chitin synthase inhibitor 4

    Fungal Infection
    Chitin synthase inhibitor 4 (compound 4fh) is a chitin synthase (CHS) inhibitor with fungicidal effect. Chitin synthase inhibitor 4 is a potential CHS-based fungicide in agriculture.
  • HY-101791
    P-gp inhibitor 1

    P-glycoprotein Cancer
    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  • HY-150570
    Carbonic anhydrase inhibitor 14

    Carbonic Anhydrase CDK Cancer
    Carbonic anhydrase inhibitor 14 (Compound 8b) is a carbonic anhydrase (CA) inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 14 can also inhibit CDK2 with an IC50 of 20.3 μM. Carbonic anhydrase inhibitor 14 shows antitumor activity.
  • HY-146316
    Topoisomerase II inhibitor 6

    Topoisomerase Cancer
    Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases.
  • HY-147649
    Glyoxalase I inhibitor 7

    Others Cancer
    Glyoxalase I inhibitor 7 (Compound 6) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 3.65 μM. Glyoxalase I inhibitor 7 can be used as anticancer agent.
  • HY-144376
    Carbonic anhydrase inhibitor 4

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 4 is carbonic anhydrase photoprobe/inhibitor. Carbonic anhydrase inhibitor 4 is against human carbonic anhydrases (hCA I-XIV) with Ki values of 640-1166 nM.
  • HY-147877
    Topoisomerase II inhibitor 12

    Topoisomerase Cancer
    Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity.
  • HY-114309
    URAT1 inhibitor 1

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.
  • HY-147647
    Glyoxalase I inhibitor 5

    Others Cancer
    Glyoxalase I inhibitor 5 (Compound 9h) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.28 μM. Glyoxalase I inhibitor 5 can be used as anticancer agent.
  • HY-50670
    DGAT-1 inhibitor 2

    Acyltransferase Metabolic Disease
    DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.
  • HY-13275
    IRAK inhibitor 1

    IRAK Inflammation/Immunology
    IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
  • HY-151416
    Chitin synthase inhibitor 6

    Fungal Infection
    Chitin synthase inhibitor 6 (compound 9b) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.21 mM. Chitin synthase inhibitor 6 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 6 can be used in the research of fungi infection.
  • HY-115994
    Carbonic anhydrase inhibitor 10

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research.
  • HY-151417
    Chitin synthase inhibitor 7

    Fungal Infection
    Chitin synthase inhibitor 7 (compound 9c) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.37 mM. Chitin synthase inhibitor 7 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 7 can be used in the research of fungi infection.
  • HY-146386
    SIRT5 inhibitor 2

    Sirtuin Cancer Neurological Disease
    SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases.
  • HY-146437
    Topoisomerase I inhibitor 6

    Topoisomerase Cancer
    Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases.
  • HY-146037
    Aurora A inhibitor 2

    Apoptosis Aurora Kinase Cancer
    Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells.
  • HY-146654
    Glyoxalase I inhibitor 2

    Others Cancer
    Glyoxalase I inhibitor 2 (compound 26) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.5 µM. Glyoxalase I inhibitor 2 has the potential for the research of depression and anxiety.
  • HY-151420
    Chitin synthase inhibitor 10

    Fungal Cancer Infection
    Chitin synthase inhibitor 10 is a chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 10 shows excellent CHS inhibitory activity with an IC50 value of 0.11 mM. Chitin synthase inhibitor 10 also is an antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 10 can be used for the research of invasive fungal infections (IFIs).
  • HY-10644
    Lck inhibitor 2

    Src Inflammation/Immunology
    Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively
  • HY-112634
    SIRT5 inhibitor 1

    Sirtuin Others
    SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
  • HY-146656
    Glyoxalase I inhibitor 4

    Others Cancer
    Glyoxalase I inhibitor 4 (compound 14) is a potent glyoxalase I inhibitor with an Ki of 10 nM.
  • HY-144988
    CD38 inhibitor 2

    Others Cancer
    CD38 inhibitor 2 is a potent CD38 inhibitor (IC50 = 0.01 ~ 0.1 μΜ).
  • HY-111493
    LRRK2 inhibitor 1

    LRRK2 Neurological Disease
    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8.
  • HY-147812
    POLA1 inhibitor 1

    Others Cancer
    POLA1 inhibitor 1 (Compound 12) is an orally active POLA1 inhibitor. POLA1 inhibitor 1 shows antitumor activity against several tumor histotypes and Adarotene-resistant cell line.
  • HY-147648
    Glyoxalase I inhibitor 6

    Others Cancer
    Glyoxalase I inhibitor 6 (Compound 9j) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.13 μM. Glyoxalase I inhibitor 6 can be used as anticancer agent with low toxicity.
  • HY-146655
    Glyoxalase I inhibitor 3

    Others Cancer
    Glyoxalase I inhibitor 3 (compound 22g) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.011 µM. Glyoxalase I inhibitor 3 has the potential for the research of depression and anxiety.
  • HY-146163
    Topoisomerase II inhibitor 7

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis.
  • HY-151410
    Chitin synthase inhibitor 5

    Fungal Infection
    Chitin synthase inhibitor 5 (compound 9a) is an inhibitor of chitin synthase with an IC50 value of 0.14 mM. Chitin synthase inhibitor 5 shows broad-spectrum antifungal activity in vitro and shows good inhibition to C. albicans, A. flavus, A. fumigatus and C. neoformans. Chitin synthase inhibitor 5 can be used for the research of fungal.
  • HY-132175
    CK2 inhibitor 2

    Casein Kinase Cancer
    CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
  • HY-151422
    Chitin synthase inhibitor 12

    Others Cancer Infection
    Chitin synthase inhibitor 12 is a chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 12 shows excellent CHS inhibitory activity with an IC50 value of 0.16 mM. Chitin synthase inhibitor 12 also is a broad-spectrum antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 12 can be used for the research of invasive fungal infections (IFIs).
  • HY-123538
    GRK2 Inhibitor 1

    Others Cardiovascular Disease
    GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a GRK2 (β-ARK1) inhibitor.
  • HY-115998
    Carbonic anhydrase inhibitor 11

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 11 (compound VI) is a potent, selective carbonic anhydrase inhibitor. Carbonic anhydrase inhibitor 11 shows Ki values of 40, 39, 200 and 900 nM against CA II, IX, and XII, respectively.
  • HY-150775
    Nonsteroidal aromatase inhibitor 1

    Aromatase Cancer
    Nonsteroidal aromatase inhibitor 1 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). Nonsteroidal aromatase inhibitor 1 has potential for breast cancer research.
  • HY-146455
    DPP-4 inhibitor 3

    Dipeptidyl Peptidase ROS Kinase Metabolic Disease
    DPP-4 inhibitor 3 (Compound 5a) is a potent dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 0.75 nM. DPP-4 inhibitor 3 shows excellent antioxidant and insulinotropic activity.
  • HY-112715
    ATP synthase inhibitor 1

    ATP Synthase Cardiovascular Disease
    ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels.
  • HY-129167
    Menin-MLL inhibitor 4

    Epigenetic Reader Domain Cancer
    Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction extracted from patent WO2017214367, compound example 1. Menin-MLL inhibitor 4 has antitumor activity.
  • HY-22166
    Glycolic acid oxidase inhibitor 1

    Others Metabolic Disease
    Glycolic acid oxidase inhibitor 1 is a glycolate oxidase inhibitor, extracted from patent EP0021228A1, in Table IV.
  • HY-143281
    Topoisomerase II inhibitor 5

    Topoisomerase Cancer
    Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer activities.
  • HY-143306
    IDH1 Inhibitor 5

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively.
  • HY-144391
    Chitin synthase inhibitor 1

    Fungal Antibiotic Inflammation/Immunology
    Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor (IC50=0.12 mM). Chitin synthase inhibitor 1 has potent antifungal activity against drug-resistant fungi variants.
  • HY-114418
    MMP3 inhibitor 1

    MMP Cancer
    MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM.
  • HY-P1258
    PSI

    Proteasome inhibitor 1

    Proteasome Cancer Infection
    PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas.
  • HY-135899
    SIRT7 inhibitor 97491

    Sirtuin Apoptosis Cancer
    SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
  • HY-143246
    EGFR kinase inhibitor 1

    EGFR Apoptosis Cancer
    EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.
  • HY-128798
    Menin-MLL inhibitor 20

    Epigenetic Reader Domain Cancer
    Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, Intermediate 6).
  • HY-146653
    Glyoxalase I inhibitor 1

    Others Cancer
    Glyoxalase I inhibitor 1 (compound 23) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 26 nM.
  • HY-112297
    BACE-1 inhibitor 1

    Beta-secretase Neurological Disease
    BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM.
  • HY-100231
    Cathepsin inhibitor 1

    Cathepsin Cancer
    Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively.
  • HY-146189
    Topoisomerase II inhibitor 9

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells.
  • HY-15735
    c-Met inhibitor 1

    c-Met/HGFR Cancer
    c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
  • HY-103032
    Multi-kinase inhibitor 1

    PDGFR c-Kit Bcr-Abl Cancer
    Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
  • HY-13335
    PKCβ inhibitor 1

    PKC Apoptosis Cancer
    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
  • HY-150583
    Chitin synthase inhibitor 2

    Fungal Antibiotic Inflammation/Immunology
    Chitin synthase inhibitor 2 (compound 2b) is a potent inhibitor of chitin synthase with the IC50 value of 0.09 mM and the Ki value of 0.12 mM. Chitin synthase inhibitor 2 has antimicrobial activities in vitro and shows synergistic or additive effects with fluconazole or polyoxin B.
  • HY-N144114
    P-gp inhibitor 2

    P-glycoprotein Cancer
    P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC50=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300).
  • HY-147031
    JAMM protein inhibitor 2

    Others Cancer
    JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2, respectively. JAMM protein inhibitor 2 can be used for researching anticancer
  • HY-146188
    Topoisomerase II inhibitor 8

    Topoisomerase Cancer
    Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase.
  • HY-151372
    Protein kinase D inhibitor 1

    PKD Cancer
    Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation.
  • HY-112432
    GlyT1 Inhibitor 1

    GlyT Neurological Disease
    GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC50 of 38 nM for rGlyT1. Antipsychotic activity.
  • HY-126142
    Top1 inhibitor 1

    Topoisomerase ADC Cytotoxin Cancer
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM.
  • HY-112701
    CCR6 inhibitor 1

    CCR Cancer Inflammation/Immunology Endocrinology
    CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.
  • HY-146504
    Topoisomerase I/II inhibitor 3

    Topoisomerase PI3K Apoptosis ROS Kinase Cancer
    Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.
  • HY-145825
    Mcl-1 inhibitor 7

    Bcl-2 Family Cancer
    Mcl-1 inhibitor 7 is a potent Mcl-1 inhibitor, example 35, extracted from patent WO2020097577A.
  • HY-126146
    PKC-iota inhibitor 1

    PKC Cancer
    PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ℩) inhibitor with an IC50 value of 0.34 μM.
  • HY-149002
    Topoisomerase I/II inhibitor 4

    Topoisomerase Apoptosis Cancer
    Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
  • HY-139076
    Menin-MLL inhibitor 19

    Epigenetic Reader Domain Cancer Metabolic Disease
    Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 can be used for the reseaech of various diseases, such as cancer, myelodysplastic syndrome (MDS) and diabetes.
  • HY-143266
    Topoisomerase I inhibitor 3

    Topoisomerase Apoptosis Cancer
    Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.
  • HY-114147
    Tuberculosis inhibitor 3

    Bacterial Infection Inflammation/Immunology
    Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 µg/mL) against drug-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability.
  • HY-147908
    Adenosine receptor inhibitor 2

    Adenosine Receptor Inflammation/Immunology
    Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR.
  • HY-147907
    Adenosine receptor inhibitor 1

    Adenosine Receptor Cancer Inflammation/Immunology Neurological Disease
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
  • HY-150565
    P-gp inhibitor 5

    P-glycoprotein Cancer
    P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
  • HY-111623
    USP30 inhibitor 11

    Deubiquitinase Cancer
    USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.
  • HY-112569
    MAT2A inhibitor 2

    Others Cancer
    MAT2A inhibitor 2 is a methionine adenosyltransferase 2A (MAT2A) inhibitor.
  • HY-147861
    Topoisomerase II inhibitor 11

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity.
  • HY-147839
    Topoisomerase II inhibitor 10

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells.
  • HY-122700
    Factor D inhibitor 6

    Complement System Inflammation/Immunology
    Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
  • HY-147940
    TbPTR1 inhibitor 1

    Parasite Infection
    TbPTR1 inhibitor 1 (compound 5d) is a potent kinetoplastid pteridine reductase 1 (PTR1) inhibitor with an IC50<0.1 nM for TbPTR1. TbPTR1 inhibitor 1 has inhibitory activity against Trypanosoma brucei (EC50=0.66 μM).
  • HY-130254
    Src Inhibitor 3

    Src Cancer Inflammation/Immunology
    Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
  • HY-143657
    Myoferlin inhibitor 1

    Others Cancer
    Myoferlin inhibitor 1 is a novel agent against pancreatic cancer metastasis through targeting myoferlin.
  • HY-131068
    BACE-1 inhibitor 2

    Beta-secretase Neurological Disease
    BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay.
  • HY-144807
    Carbonic anhydrase inhibitor 9

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity.
  • HY-150044
    Type II topoisomerase inhibitor 1

    DNA/RNA Synthesis Topoisomerase Bacterial Infection
    Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
  • HY-11059
    sPLA2 inhibitor 1

    Phospholipase Inflammation/Immunology
    sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity.
  • HY-143713
    Aurora A inhibitor 1

    Aurora Kinase Cancer
    Aurora A inhibitor 1 is a potent and selective inhibitor of Aurora A. Aurora A has been implicated in cancers of diverse histological origin and may possess oncogenic properties when overexpressed. Aurora A inhibitor 1 has the potential for the research of cancer diseases mediated by aurora a (extracted from patent WO2021147974A1, compound 49).
  • HY-147785
    Pim-1 kinase inhibitor 2

    Pim Apoptosis Cancer
    Pim-1 kinase inhibitor 2 (Compound 13) is a potent inhibitor of Pim-1 kinase. Pim-1 kinase inhibitor 2 induces apoptosis. Pim-1 kinase inhibitor 2 has the potential for the research of cancer diseases.
  • HY-U00387
    CCK-A receptor inhibitor 1

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    CCK-A receptor inhibitor 1 is a cholecystokinin A (CCK-A) receptor inhibitor with a binging IC50 of 340 nM.
  • HY-128661
    IDH1 Inhibitor 2

    Isocitrate Dehydrogenase (IDH) Metabolic Disease
    IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
  • HY-139536
    MAT2A inhibitor 4

    Others Cancer
    MAT2A inhibitor 4 is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A). MAT2A inhibitor 4 can be used for the research of cancer.
  • HY-132307
    Mcl-1 inhibitor 6

    Bcl-2 Family Apoptosis Cancer
    Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
  • HY-146227
    DNA topoisomerase II inhibitor 1

    Topoisomerase Apoptosis Cancer
    DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase.
  • HY-132920
    KRAS mutant protein inhibitor 1

    Ras Cancer
    KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer.
  • HY-U00304
    Aurora B inhibitor 1

    Aurora Kinase Cancer
    Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM.
  • HY-138989
    15-LOX-1 inhibitor 1

    Lipoxygenase Inflammation/Immunology
    15-LOX-1 inhibitor 1 is a potent inhibitor of 15-LOX-1 (15-lipoxygenase-1) with an IC50 value of 0.19 μM. 15-LOX-1 inhibitor 1 protects macrophages from lipopolysaccharide-induced cytotoxicity. 15-LOX-1 inhibitor 1 inhibits NO formation and lipid peroxidation.
  • HY-142452
    Pan-RAF kinase inhibitor 1

    Others Cancer
    Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B).
  • HY-143793
    RBP4 inhibitor 1

    Others Metabolic Disease
    RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice.
  • HY-143714
    Cathepsin K inhibitor 2

    Cathepsin Inflammation/Immunology
    Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).
  • HY-129189
    RAS GTPase inhibitor 1

    Ras Cancer
    RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
  • HY-133015
    Mcl-1 inhibitor 3

    Bcl-2 Family Cancer
    Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.
    .
  • HY-103673
    AMPD2 inhibitor 1

    Adenosine Deaminase Neurological Disease
    AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in the research of sugar craving, salt craving, umami craving, and addictions including drug, tobacco, nicotine and alcohol addictions.
  • HY-150584
    Chitin synthase inhibitor 3

    Fungal Infection
    Chitin synthase inhibitor 3 (compound 2d) is a potent chitin synthase inhibitor with an IC50 value of 0.16 mM, and MIC of 1 µg/mL against candida albicans. Antifungal activity.
  • HY-107977
    IDH1 Inhibitor 3

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1 R132H.
  • HY-150727
    SIRT5 inhibitor 4

    Sirtuin Cancer
    SIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively.
  • HY-123999
    CD38 inhibitor 1

    Others Metabolic Disease
    CD38 inhibitor 1 (compound 78c) is a potent CD38 inhibitor with IC50s of 7.3 nM and 1.9 nM for hCD38 and mouse CD38.
  • HY-111507
    PDGFRα kinase inhibitor 1

    PDGFR Cancer
    PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
  • HY-150079
    HIV-1 integrase inhibitor 10

    HIV Integrase Infection
    HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).
  • HY-131061
    BET bromodomain inhibitor 1

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
  • HY-128888
    WT IDH1 Inhibitor 2

    Isocitrate Dehydrogenase (IDH) Cancer
    WT IDH1 Inhibitor 2 (Compound 3) is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. WT IDH1 Inhibitor 2 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity.
  • HY-107485
    HIV-1 integrase inhibitor 8

    HIV Integrase Infection
    HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8.
  • HY-100257
    Sodium Channel inhibitor 2

    Sodium Channel Neurological Disease
    Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.
  • HY-147644
    α-Synuclein inhibitor 3

    Others Neurological Disease
    α-Synuclein inhibitor 3 (Compound 7g) is a α-synuclein (α -Syn) aggregation inhibitor. α-Synuclein inhibitor 3 can be used for Parkinson’s disease research.
  • HY-112441
    Prolyl Hydroxylase inhibitor 1

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent.
  • HY-101998
    CTP inhibitor

    Others Metabolic Disease
    CTP inhibitor is a potent and selective CTP inhibitor. CTP inhibitor inhibits the plasma membrane citrate transporter (PMCT).
  • HY-116044
    BCATc Inhibitor 2

    Others Neurological Disease
    BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively. BCATc, also called BCAT1, is in the cytoplasm.
  • HY-100556
    Tie2 kinase inhibitor 1

    Others Cancer
    Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
  • HY-136010
    RIP2 Kinase Inhibitor 4

    RIP kinase PROTACs Inflammation/Immunology
    RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α.
  • HY-115213
    SORT-PGRN interaction inhibitor 1

    Neurotensin Receptor Neurological Disease
    SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC50 of 2 μM.
  • HY-147633
    KRAS G12C inhibitor 52

    Ras Cancer
    KRAS G12C inhibitor 52 (Compound 7) is a KRAS G12C inhibitor.
  • HY-147636
    KRAS G12C inhibitor 55

    Ras Cancer
    KRAS G12C inhibitor 55 (Compound 1) is a KRAS G12C inhibitor.
  • HY-147632
    KRAS G12C inhibitor 51

    Ras Cancer
    KRAS G12C inhibitor 51 (example 1) is a KRAS G12C inhibitor.
  • HY-147635
    KRAS G12C inhibitor 54

    Ras Cancer
    KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor.
  • HY-147634
    KRAS G12C inhibitor 53

    Ras Cancer
    KRAS G12C inhibitor 53 (Compound 1) is a KRAS G12C inhibitor.
  • HY-132572
    HIV-1 integrase inhibitor 9

    HIV Infection
    HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity.
  • HY-114423
    p38α inhibitor 1

    p38 MAPK Autophagy Inflammation/Immunology
    p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
  • HY-144639
    Carbonic anhydrase inhibitor 5

    Carbonic Anhydrase Cancer Infection Inflammation/Immunology
    Carbonic anhydrase inhibitor 5 is a potent and selective human carbonic anhydrase (hCA) inhibitor with IC50s of 42.9, 47,6 and 6.7 nM for hCA II, hCA IX and hCA XII, respectively.
  • HY-139139
    MAT2A inhibitor 3

    Others Cancer
    MAT2A inhibitor 3 is a methionine adenosyltransferase 2A (MAT2A) inhibitor extracted from patent WO2020123395A1, compound 24, has an IC50 of <200 nM. MAT2A inhibitor 3 can be used for the research of cancers.
  • HY-142947
    KRAS G12C inhibitor 45

    Ras Cancer
    KRAS G12C inhibitor 45 (compound 78) is a potent KRAS G12C inhibitor.
  • HY-130795
    GSK-3β inhibitor 2

    GSK-3 Neurological Disease
    GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
  • HY-143295
    Pim-1 kinase inhibitor 1

    Pim Apoptosis Cancer
    Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC50 of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer.
  • HY-114313
    Microtubule inhibitor 1

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells.
  • HY-108820
    HIV-1 integrase inhibitor 4

    HIV Integrase HIV Infection
    HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
  • HY-108817
    HIV-1 integrase inhibitor 3

    HIV Integrase HIV Infection
    HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.
  • HY-139686
    IL-17A inhibitor 2

    Interleukin Related Inflammation/Immunology
    IL-17A inhibitor 2 is an IL-17A inhibitor for treating psoriasis, rheumatoid arthritis, and multiple sclerosis.
  • HY-143279
    Topoisomerase II inhibitor 3

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential.
  • HY-115990
    Topoisomerase IV inhibitor 1

    Topoisomerase Bacterial Infection
    Topoisomerase IV inhibitor 2 (compound 7d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.23 μM and 0.43 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 0.972 μM and 0.608 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
  • HY-115991
    Topoisomerase IV inhibitor 2

    Topoisomerase Bacterial Infection
    Topoisomerase IV inhibitor 2 (compound 5d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.35 μM and 0.55 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 1.985 μM and 0.744 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
  • HY-143906
    URAT1 inhibitor 2

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising drug candidate in the study of hyperuricemia and gout.
  • HY-142948
    KRAS G12C inhibitor 46

    Ras Cancer
    KRAS G12C inhibitor 46 (compound WX003) is a potent KRAS G12C inhibitor.
  • HY-143245
    Monoamine Oxidase B inhibitor 2

    Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
  • HY-143244
    Monoamine Oxidase B inhibitor 1

    Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
  • HY-115984
    Carbonic anhydrase inhibitor 8

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 8 (compound R-13), a benzyl-derivative, is a potent human carbonic anhydrase (hCA) inhibitor with Ki values of 60.7 nM, 320.7 nM, 2298 nM for hCA I, hCA II, hCA IV, respectively.
  • HY-112722
    Neurotoxin Inhibitor

    Others Neurological Disease
    Neurotoxin Inhibitor is a neurotoxin inhibitor.
  • HY-124832
    δ-Secretase inhibitor 11

    Caspase Amyloid-β Neurological Disease
    δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research.
  • HY-112131
    MAT2A inhibitor 1

    Others Cancer
    MAT2A inhibitor 1 is a methionine adenosyltransferase 2A (MATA2) inhibitor with an IC50 less than l00 nM.
  • HY-130760
    HIV-1 integrase inhibitor 7

    HIV Integrase Infection
    HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC50 of 33.3 nM.
  • HY-15736
    Sodium Channel inhibitor 1

    Sodium Channel Neurological Disease
    Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
  • HY-133014
    RIP2 kinase inhibitor 1

    RIP kinase Inflammation/Immunology
    RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders.
  • HY-145020
    KRAS G12C inhibitor 23

    Ras Cancer
    KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1).
  • HY-146010
    Carbonic anhydrase inhibitor 13

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 13 (compound 7) is a potent carbonic anhydrase (CA) inhibitor, which features 3-methylthiazolo[3,2-a]benzimidazole moiety (as a tail) connected to the zinc anchoring benzenesulfonamide moiety via ureido linker.
  • HY-144641
    Carbonic anhydrase inhibitor 7

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 7 (compound 5b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 6.5 nM, 7.1 nM, 72.1 nM, and 255.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively.
  • HY-144640
    Carbonic anhydrase inhibitor 6

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 6 (compound 9b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 9.7 nM, 35.2 nM, 88.5 nM, and 91.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively.
  • HY-146391
    P-gp inhibitor 4

    P-glycoprotein Cancer
    P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
  • HY-132980
    KRAS G12C inhibitor 19

    Ras Cancer
    KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1).
  • HY-142487
    KRAS G12C inhibitor 32

    Ras Cancer
    KRAS G12C inhibitor 32, an eight membered heterocyclic compound containing N, is a potent KRAS G12C inhibitor.
  • HY-147134
    GSK-3β inhibitor 10

    GSK-3 Neurological Disease
    GSK-3β inhibitor 10 (compound 14a) is a highly potent GSK-3β inhibitor with an IC50 value of 80.5 nM. GSK-3β inhibitor 10 can be used for researching Alzheimer’s disease.
  • HY-112907
    RIP2 Kinase Inhibitor 3

    RIP kinase Inflammation/Immunology
    RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC50 of 1 nM .
  • HY-12444
    Y15

    FAK inhibitor 14

    FAK Cancer
    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
  • HY-143260
    GSK-3β inhibitor 6

    GSK-3 Cancer Metabolic Disease Inflammation/Immunology
    GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
  • HY-131335
    p38α inhibitor 2

    p38 MAPK Inflammation/Immunology
    p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
  • HY-19762
    GSK1940029

    SCD inhibitor 1

    Stearoyl-CoA Desaturase (SCD) Cancer
    GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16.
  • HY-142437
    ERK1/2 inhibitor 8

    ERK Cancer
    ERK1/2 inhibitor 8 is a potent ERK inhibitor with an IC50 of 0.48 nM for ERK2 (WO2021110168A1, WX007).
  • HY-142433
    ERK1/2 inhibitor 7

    ERK Cancer
    ERK1/2 inhibitor 7 is a potent ERK inhibitor with an IC50 of 0.94 nM for ERK2 (WO2021110168A1, WX006).
  • HY-150731
    Pim-1 kinase inhibitor 3

    Pim Cancer
    Pim-1 kinase inhibitor 3 (Compound H5) is a potent Pim-1 kinase inhibitor with an IC50 of 35.13 nM.
  • HY-139885
    c-Myc inhibitor 4

    c-Myc Cancer
    c-Myc inhibitor 4 is a potent, orally bioavailable c-MYC-reducing compound.
  • HY-115510
    SPR inhibitor 3

    SPRi3

    Others Inflammation/Immunology
    SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
  • HY-114414
    HDACs/mTOR Inhibitor 1

    HDAC mTOR Apoptosis Cancer
    HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
  • HY-13277
    IRAK inhibitor 3

    IRAK Inflammation/Immunology
    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  • HY-12202
    MEK inhibitor

    MEK Cancer
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
  • HY-111409
    RIP1 kinase inhibitor 1

    RIP kinase Inflammation/Immunology
    RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04).
  • HY-141480
    GSK-3β inhibitor 3

    GSK-3 Apoptosis Cancer
    GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.
  • HY-145021
    KRAS G12C inhibitor 24

    Ras Cancer
    KRAS G12C inhibitor 24 is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 24 inhibits KRAS G12C/SOS1 interaction with an IC50 of<50 nM (CN113563323A, compound 1).
  • HY-101282
    Glutaminyl Cyclase Inhibitor 3

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.
  • HY-145843
    c-Myc inhibitor 5

    c-Myc Cancer
    c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes.
  • HY-19761
    RIP2 kinase inhibitor 2

    RIP kinase Cancer
    RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
  • HY-17542
    PLpro inhibitor

    SARS-CoV Infection
    PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
  • HY-143261
    GSK-3β inhibitor 7

    GSK-3 Cancer Metabolic Disease Inflammation/Immunology
    GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC50 value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
  • HY-145022
    KRAS G12C inhibitor 25

    Ras Cancer
    KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3.
  • HY-147630
    KRAS G12C inhibitor 49

    Ras Cancer
    KRAS G12C inhibitor 49 (Compound 3-2M) is an orally active KRAS G12C inhibitor. KRAS G12C inhibitor 49 shows antitumor activity.
  • HY-139894
    KRAS G12D inhibitor 5

    Ras Cancer
    KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential treatment of pancreatic cancer.
  • HY-124594
    CA inhibitor 1

    GS-6207 analog

    HIV Infection
    CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition.
  • HY-139206
    IL-17A inhibitor 1

    Interleukin Related Inflammation/Immunology
    IL-17A inhibitor 1 (example 24) is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells.
  • HY-150003
    Aβ1–42 aggregation inhibitor 1

    Others Neurological Disease
    Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC50 value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease.
  • HY-W412264
    Pim-1/2 kinase inhibitor 1

    Pim Cancer
    Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer.
  • HY-142478
    KRAS G12C inhibitor 29

    Ras Cancer
    KRAS G12C inhibitor 29 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 3. KRAS G12C inhibitor 29 can be used for the research of cancer.
  • HY-142481
    KRAS G12C inhibitor 30

    Ras Cancer
    KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer.
  • HY-142485
    KRAS G12C inhibitor 31

    Ras Cancer
    KRAS G12C inhibitor 31 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer.
  • HY-142490
    KRAS G12C inhibitor 33

    Ras Cancer
    KRAS G12C inhibitor 33 is a KRAS G12C inhibitor extracted from patent WO2021244603A1, compound 1. KRAS G12C inhibitor 33 can be used for the research of cancer.
  • HY-12072
    Lck Inhibitor

    Src Inflammation/Immunology
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
  • HY-112616
    NAMPT inhibitor-linker 2

    NAMPT Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
  • HY-12358
    Tpl2 Kinase Inhibitor 1

    MAP3K Cancer Inflammation/Immunology
    Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor, plays an important role in the regulation of the inflammatory response and the progression of some cancers.
  • HY-112287
    ERK1/2 inhibitor 1

    ERK Cancer
    ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.
  • HY-142511
    KRAS G12C inhibitor 34

    Ras Cancer
    KRAS G12C inhibitor 34 is a KRAS G12C inhibitor extracted from patent WO2021239058A1, compound Z1. KRAS G12C inhibitor 34 can be used for the research of cancer.
  • HY-112601
    IDH1 Inhibitor 1

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. Anticancer activity.
  • HY-147668
    α-Synuclein inhibitor 6

    Others Neurological Disease
    α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4%.
  • HY-147666
    α-Synuclein inhibitor 4

    Others Neurological Disease
    α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2%.
  • HY-147669
    α-Synuclein inhibitor 7

    Others Neurological Disease
    α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8%.
  • HY-126144
    GSK-3β inhibitor 1

    GSK-3 Metabolic Disease
    GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.
  • HY-147667
    α-Synuclein inhibitor 5

    Others Neurological Disease
    α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3%.
  • HY-112615
    NAMPT inhibitor-linker 1

    Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
  • HY-15886
    Mdivi-1

    Mitochondrial division inhibitor 1

    Dynamin Mitophagy Autophagy Apoptosis Cancer
    Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. Mdivi-1 is a mitochondrial division/mitophagy inhibitor.
  • HY-15288
    PI3kδ inhibitor 1

    PI3K Cancer
    PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
  • HY-101766
    Btk inhibitor 2

    BGB-3111 analog

    Btk Inflammation/Immunology
    Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
  • HY-112494
    KRas G12C inhibitor 4

    Ras Cancer
    KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-112491
    KRas G12C inhibitor 1

    Ras Cancer
    KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-132979
    KRAS G12C inhibitor 18

    Ras Cancer
    KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities.
  • HY-147631
    KRAS G12C inhibitor 50

    Ras Cancer
    KRAS G12C inhibitor 50 (Example 4) is a KRAS G12C inhibitor with an IC50 of 46.7 nM.
  • HY-112493
    KRas G12C inhibitor 3

    Ras Cancer
    KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-15223
    MI-3

    Menin-MLL inhibitor 3

    Epigenetic Reader Domain Apoptosis Cancer
    MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC50 of 648 nM and a Kd of 201 nM.
  • HY-112492
    KRas G12C inhibitor 2

    Ras Cancer
    KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-145017
    KRAS G12C inhibitor 20

    Ras Cancer
    KRAS G12C inhibitor 20 is a KRAS G12C inhibitor extracted from patent CN112694475A, example 1.
  • HY-147595
    KRAS G12D inhibitor 15

    Ras Cancer
    KRAS G12D inhibitor 15 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243).
  • HY-145436
    KRAS inhibitor-11

    Ras Cancer
    KRAS inhibitor-11 (compound 12) is a KRAS inhibitor.
  • HY-145025
    ERK1/2 inhibitor 3

    ERK Cancer Inflammation/Immunology
    ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1).
  • HY-145026
    ERK1/2 inhibitor 4

    ERK Cancer Inflammation/Immunology
    ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1).
  • HY-145027
    ERK1/2 inhibitor 5

    ERK Cancer
    ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1).
  • HY-145028
    ERK1/2 inhibitor 6

    ERK Cancer Inflammation/Immunology
    ERK1/2 inhibitor 6 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1).
  • HY-145018
    KRAS G12C inhibitor 21

    Ras Cancer
    KRAS G12C inhibitor 21 is a KRAS G12C inhibitor extracted from patent WO2021219090A1, example 7.
  • HY-126292
    KRAS G12C inhibitor 13

    Ras Cancer
    KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.
  • HY-145019
    KRAS G12C inhibitor 22

    Ras Cancer
    KRAS G12C inhibitor 22 is a KRAS G12C inhibitor extracted from patent WO2021219072A1, example 120.
  • HY-139911
    KRAS G12D inhibitor 7

    Ras Cancer
    KRAS G12D inhibitor 7 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683, compound 114) .
  • HY-142946
    KRAS G12C inhibitor 44

    Ras Cancer
    KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo.
  • HY-114168
    KRAS G12C inhibitor 5

    Ras Cancer
    KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147.
  • HY-139910
    KRAS G12D inhibitor 6

    Ras Cancer
    KRAS G12D inhibitor 6 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683A1, compound 112) .
  • HY-139880
    PI3Kγ inhibitor 5

    PI3K Cancer
    PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.
  • HY-110247
    TRAF-STOP inhibitor 6877002

    TNF Receptor NF-κB Inflammation/Immunology Cardiovascular Disease
    TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
  • HY-132299
    PI3Kγ inhibitor 4

    PI3K Inflammation/Immunology
    PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation.
  • HY-146226
    Viral 2C protein inhibitor 1

    Enterovirus Infection
    Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity.
  • HY-10247
    BRAF inhibitor

    Raf Cancer
    BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
  • HY-144687
    ATM Inhibitor-4

    ATM/ATR PI3K mTOR Cancer
    ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability.
  • HY-115900
    Tuberculosis inhibitor 4

    Bacterial Infection
    Tuberculosis inhibitor 4 (compound 16), a mandelic acid-based spirothiazolidinone, has potent antimycobacterial activity against Mycobacterium tuberculosis strain H37Rv with the high inhibition value 98% at lower than 6.25 µg/mL concentration.
  • HY-131344
    mTOR inhibitor-8

    mTOR Autophagy Cancer
    mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
  • HY-151287
    KRAS inhibitor-20

    Ras Cancer
    KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM.
  • HY-144686
    ATM Inhibitor-3

    ATM/ATR PI3K mTOR Cancer
    ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability.
  • HY-146537
    KRAS G12C inhibitor 47

    Ras Cancer
    KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-P3442
    KRAS inhibitor-19

    Ras Cancer
    KRAS inhibitor-19 KRAS inhibitor-19 (Peptide 7) is a potent KRAS inhibitor (IC50=3.8 μM) and also inhibits pERK activity in a KRAS G12D pancreatic cancer cell line. KRAS inhibitor-19 KRAS inhibitor-19 (Peptide 7) has the binding affinity and cellular activity in a KRAS G12D pancreatic cancer cell line and no LDH release or activity in A375 cells.
    .
  • HY-W018931
    DDR Inhibitor

    Discoidin Domain Receptor Cancer
    DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
  • HY-142945
    KRAS G12C inhibitor 43

    Ras Cancer
    KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively.
  • HY-77048
    IRAK-4 protein kinase inhibitor 2

    IRAK Inflammation/Immunology
    IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM. IRAK-4 protein kinase inhibitor 2 can be used for the research of inflammatory and immune-related conditions or disorders.
  • HY-112286
    PI3Kγ inhibitor 2

    PI3K Inflammation/Immunology
    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  • HY-112439
    PI3Kdelta inhibitor 1

    PI3K Cancer Inflammation/Immunology
    PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
  • HY-139607
    SSAO inhibitor-1

    Monoamine Oxidase Inflammation/Immunology
    SSAO inhibitor-1 is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor. SSAO inhibitor-1 has anti-inflammatory activity and can be used for liver diseases research.
  • HY-126144A
    (E/Z)-GSK-3β inhibitor 1

    GSK-3 Metabolic Disease
    (E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers. GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.
  • HY-125873
    KRAS G12C inhibitor 15

    Ras Cancer
    KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM.
  • HY-125875
    KRAS G12C inhibitor 17

    Ras Cancer
    KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM.
  • HY-125874
    KRAS G12C inhibitor 16

    Ras Cancer
    KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM.
  • HY-125872
    KRAS G12C inhibitor 14

    Ras Cancer
    KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 17, has an IC50 of 18 nM.
  • HY-18353
    mTOR inhibitor-3

    mTOR Cancer
    mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
  • HY-151288
    KRAS inhibitor-21

    Ras Cancer
    KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC50 value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research.
  • HY-147374
    Bromodomain inhibitor-9

    Epigenetic Reader Domain Metabolic Disease Inflammation/Immunology
    Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases.
  • HY-150963
    Renin inhibitor-1

    Renin Cardiovascular Disease
    Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC50s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases.
  • HY-70003
    Carboxypeptidase G2 (CPG2) Inhibitor

    CPG2 inhibitor

    Carboxypeptidase Cancer
    Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
  • HY-143592
    KRAS G12C inhibitor 39

    Ras Cancer
    KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494).
  • HY-144661
    KRAS G12D inhibitor 14

    Ras Apoptosis Cancer
    KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.
  • HY-137497
    KRAS inhibitor-9

    Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
  • HY-134811
    KRAS G12D inhibitor 1

    Ras Cancer
    KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation.
  • HY-147375
    Bromodomain inhibitor-10

    Epigenetic Reader Domain Cancer
    Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40.
  • HY-139648
    PREP inhibitor-1

    Prolyl Endopeptidase (PREP) Others
    PREP inhibitor-1 is a highly potent prolyl oligopeptidase (PREP) inhibitor (IC50 < 1 nM).
  • HY-143588
    KRAS G12C inhibitor 35

    Ras Cancer
    KRAS G12C inhibitor 35 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 35 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent CN112920183A, compound 3).
  • HY-143294
    sEH inhibitor-2

    Epoxide Hydrolase Cardiovascular Disease
    sEH inhibitor-2 (compound 5l) is an orally active (predicted percentage absorption: 71.2-88.4%) soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 0.9 nM. sEH inhibitor-2 can maintain epoxyeicosatrienoic acids (EETs) serum level in high concentrations. sEH inhibitor-2 can be used in study of cardiovascular protection.
  • HY-111370
    mTOR inhibitor-2

    mTOR Cancer
    mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
  • HY-101275
    EMT inhibitor-1

    Hippo (MST) TGF-beta/Smad Wnt Cancer
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-112605
    sPLA2-X Inhibitor 31

    Phospholipase Cardiovascular Disease
    sPLA2-X Inhibitor 31 is a selective secreted phospholipase A2 type X (sPLA2-X) inhibitor with IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively.
  • HY-143590
    KRAS G12C inhibitor 37

    Ras Cancer
    KRAS G12C inhibitor 37 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 37 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2018143315A1, compound 65).
  • HY-143606
    KRAS G12D inhibitor 12

    Ras Cancer
    KRAS G12D inhibitor 12 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 134).
  • HY-143594
    KRAS G12C inhibitor 40

    Ras Cancer
    KRAS G12C inhibitor 40 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 40 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 70).
  • HY-146061
    KRAS G12C inhibitor 48

    Ras Cancer
    KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively.
  • HY-143604
    KRAS G12D inhibitor 11

    Ras Cancer
    KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 11 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 52).
  • HY-143591
    KRAS G12C inhibitor 38

    Ras Cancer
    KRAS G12C inhibitor 38 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 38 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129820A1, compound 171).
  • HY-143589
    KRAS G12C inhibitor 36

    Ras Cancer
    KRAS G12C inhibitor 36 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 36 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1, compound 1-2).
  • HY-143598
    KRAS G12C inhibitor 42

    Ras Cancer
    KRAS G12C inhibitor 42 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 42 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2020146613A1, compound 10).
  • HY-143599
    KRAS G12D inhibitor 8

    Ras Cancer
    KRAS G12D inhibitor 8 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 8 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021107160A1, compound 2).
  • HY-143607
    KRAS G12D inhibitor 13

    Ras Cancer
    KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142).
  • HY-143602
    KRAS G12D inhibitor 9

    Ras Cancer
    KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20).
  • HY-143596
    KRAS G12C inhibitor 41

    Ras Cancer
    KRAS G12C inhibitor 41 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 41 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 121).
  • HY-143603
    KRAS G12D inhibitor 10

    Ras Cancer
    KRAS G12D inhibitor 10 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 10 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 34).
  • HY-147388
    hiCE inhibitor-1

    Others Metabolic Disease
    hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea.
  • HY-111412
    DAAO inhibitor-1

    Others Neurological Disease
    DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC50 of 0.12 μM.
  • HY-12446
    K-Ras(G12C) inhibitor 9

    Ras Cancer
    K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C).
  • HY-138295
    KRAS inhibitor-10

    Ras Cancer
    KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
  • HY-112914
    mTOR inhibitor-1

    mTOR Autophagy Cancer
    mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
  • HY-144685
    ATM Inhibitor-2

    ATM/ATR Cancer
    ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nM.
  • HY-130260
    KRAS inhibitor-4

    Ras Cancer
    KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents.
  • HY-128703
    Bromodomain inhibitor-8

    Epigenetic Reader Domain Inflammation/Immunology
    Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.
  • HY-142444
    SSAO/VAP-1 inhibitor 1

    Others Metabolic Disease
    SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).
  • HY-139605
    GLUT inhibitor-1

    GLUT Cancer Inflammation/Immunology
    GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases.
  • HY-P1258A
    PSI TFA

    Proteasome inhibitor 1 TFA

    Proteasome Cancer Infection
    PSI (TFA) is a potent proteasome inhibitor. PSI (TFA) inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI (TFA) can be used for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas.
  • HY-15535
    DMAT

    CK2 inhibitor; Casein kinase II inhibitor

    Casein Kinase Cancer
    DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
  • HY-15679
    PI4KIII beta inhibitor 3

    PI4K Cancer
    PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
  • HY-112807
    SGLT inhibitor-1

    SGLT Metabolic Disease
    SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
  • HY-17541A
    Cysteine Protease inhibitor hydrochloride

    Cathepsin Others
    Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
  • HY-17541
    Cysteine Protease inhibitor

    Cathepsin Others
    Cysteine Protease inhibitor is an inhibitor of cysteine protease.
  • HY-146543
    KRAS inhibitor-13

    Ras Cancer
    KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-146533
    KRAS inhibitor-12

    Ras Cancer
    KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-146545
    KRAS inhibitor-15

    Ras Cancer
    KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-146476
    KRAS inhibitor-18

    Ras Cancer
    KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-146546
    KRAS inhibitor-16

    Ras Cancer
    KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-146475
    KRAS inhibitor-17

    Ras Cancer
    KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-146544
    KRAS inhibitor-14

    Ras Cancer
    KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers.
  • HY-111752
    EML4-ALK kinase inhibitor 1

    Anaplastic lymphoma kinase (ALK) Cancer
    EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
  • HY-32015
    Cot inhibitor-1

    MAP3K Inflammation/Immunology
    Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
  • HY-128859
    EMT inhibitor-2

    Cytochrome P450 Metabolic Disease
    EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
  • HY-10421
    Tyrosine kinase inhibitor

    c-Met/HGFR Cancer
    Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor.
  • HY-18707
    K-Ras(G12C) inhibitor 12

    Ras Apoptosis Cancer
    K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.
  • HY-10549
    PI3Kγ inhibitor 1

    PI3K Cancer
    PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
  • HY-107841
    K-Ras(G12C) inhibitor 6

    Ras Cancer
    K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C).
  • HY-148000
    sEH inhibitor-6

    Epoxide Hydrolase Inflammation/Immunology Cardiovascular Disease
    sEH inhibitor-6 (Compound 3g) is a soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 0.5 nM.
  • HY-112390A
    Syk Inhibitor II

    Syk 5-HT Receptor Inflammation/Immunology
    Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
  • HY-119937
    ROCK inhibitor-2

    ROCK Inflammation/Immunology Cardiovascular Disease
    ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively.
  • HY-146194
    NHEJ inhibitor-1

    Reactive Oxygen Species Cancer
    NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the  non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin。NHEJ inhibitor-1 also induces ROS generation and MMP deduction.
  • HY-32018
    Cot inhibitor-2

    MAP3K Cancer
    Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
  • HY-135864
    KRAS inhibitor-6

    Ras Cancer
    KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
  • HY-135866
    KRAS inhibitor-8

    Ras Cancer
    KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
  • HY-147733
    sEH inhibitor-5

    Cholinesterase (ChE) Inflammation/Immunology
    sEH inhibitor-5 (compound D016) is a potent sEH (soluble epoxide hydrolase) inhibitor with an IC50 value of 0.1 nM.
  • HY-146643
    sEH inhibitor-3

    Epoxide Hydrolase Neurological Disease
    sEH inhibitor-3 (compound 35) is a potent and orally active soluble epoxide hydrolase (sEH) inhibitor with a Ki of 0.75 nM for human sEH.
  • HY-135865
    KRAS inhibitor-7

    Ras Cancer
    KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
  • HY-114311
    FGFR1/DDR2 inhibitor 1

    FGFR Discoidin Domain Receptor Cancer
    FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
  • HY-15167
    Glyoxalase I inhibitor

    Others Cancer
    Glyoxalase I inhibitor is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
  • HY-142655
    Ftase inhibitor III

    Farnesyl Transferase Infection
    Ftase inhibitor III is an anion-dependent Farnesyltransferase inhibitor from a phenotypic screen.
  • HY-150617
    ATM Inhibitor-5

    ATM/ATR Cancer
    ATM Inhibitor-5 [formula (1)] is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1).
  • HY-139609
    RP-3500

    ATR inhibitor 4

    ATM/ATR mTOR Cancer
    RP-3500 (ATR inhibitor 4) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. RP-3500 shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. RP-3500 has potent antitumor activity.
  • HY-10249A
    AKT Kinase Inhibitor

    Akt Cancer
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
  • HY-100211
    TAPI-2

    TNF Protease inhibitor 2

    MMP SARS-CoV Cancer
    TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
  • HY-139629
    ANAT inhibitor-1

    Others Neurological Disease
    ANAT inhibitor-1 is a human aspartate N-acetyltransferase (ANAT) inhibitor for canavan disease.
  • HY-139630
    ANAT inhibitor-2

    Others Neurological Disease
    ANAT inhibitor-2 is a ANAT inhibitor for canavan disease, with an IC50 value of 20 μM.
  • HY-120494
    sEH inhibitor-1

    Epoxide Hydrolase Inflammation/Immunology
    sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively.
  • HY-115753
    Calpain Inhibitor-1

    Proteasome Neurological Disease
    Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC50=100 nM; Ki=2.89 μM).
  • HY-W181102
    NFAT Inhibitor-2

    Others Inflammation/Immunology Neurological Disease Cardiovascular Disease
    NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17).
  • HY-102090
    B7/CD28 interaction inhibitor 1

    Others Inflammation/Immunology
    B7/CD28 interaction inhibitor 1 (copmound 6b) is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM.
  • HY-10862
    FAAH inhibitor 1

    Benzothiazole analog 3

    FAAH Autophagy Cancer
    FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
  • HY-13984
    Mutant EGFR inhibitor

    EGFR Cancer
    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
  • HY-19763
    BEBT-908

    PI3Kα inhibitor 1

    PI3K Cancer
    BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
  • HY-P1111
    Lyn peptide inhibitor

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-112136
    TAO Kinase inhibitor 1

    CP 43

    Others MAP3K Cancer
    TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
  • HY-147708
    T-Type calcium channel inhibitor 2

    Calcium Channel Cancer
    T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively.
  • HY-147322
    YAP/TAZ inhibitor-2

    YAP Cancer
    YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity.
  • HY-133987
    AP-1/NF-κB activation inhibitor 1

    NF-κB Inflammation/Immunology
    AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
  • HY-139624
    JNK3 inhibitor-1

    JNK Others
    JNK3 inhibitor-1 is a potent and selective JNK3 inhibitor (IC50 = 0.005 μM). JNK3 inhibitor-1 is orally bioavailable and brain penetrant.
  • HY-103036
    BET bromodomain inhibitor

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
  • HY-146617
    GLS1 Inhibitor-4

    Glutaminase Apoptosis Cancer
    GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity.
  • HY-114996
    ADAMTS-5 Inhibitor

    Others Inflammation/Immunology
    ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
  • HY-146616
    GLS1 Inhibitor-3

    Glutaminase Cancer
    GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity.
  • HY-147993
    Aurora kinase inhibitor-10

    Aurora Kinase Cancer
    Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity.
  • HY-146088
    HIV-1 inhibitor-31

    HIV Infection
    HIV-1 inhibitor-31 (compound 4) is a potent HIV-1 inhibitor. HIV-1 inhibitor-31 can be used for researching AIDS.
  • HY-P2502
    Hepatitis Virus C NS3 Protease Inhibitor 2

    HCV Protease HCV Infection
    Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM.
  • HY-144991
    Aurora kinase inhibitor-8

    Aurora Kinase Cancer
    Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
  • HY-112851
    Diacylglycerol acyltransferase inhibitor-1

    Acyltransferase Metabolic Disease
    Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
  • HY-112812
    SCD1 inhibitor-1

    Stearoyl-CoA Desaturase (SCD) Cancer Metabolic Disease
    SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor.
  • HY-141525
    SCD1 inhibitor-4

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    SCD1 inhibitor-4 is a potent, orally active stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.
  • HY-142468
    HIV-1 inhibitor-12

    HIV Infection
    HIV-1 inhibitor-12 is potent HIV-1 inhibitor. HIV-1 inhibitor-12 inhibits HIV-1 capsid protein polymerization with an IC50 of 9 nM (WO2021104413A1, compound 1-1a).
  • HY-145909
    BRD4 Inhibitor-17

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.
  • HY-143272
    FGFR1 inhibitor-6

    FGFR Cancer
    FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase.
  • HY-112911
    Endothelial lipase inhibitor-1

    Others Cardiovascular Disease
    Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.
  • HY-146660
    BRD4 Inhibitor-18

    c-Myc Epigenetic Reader Domain Apoptosis Cancer
    BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity.
  • HY-146208
    BRD4 Inhibitor-20

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.
  • HY-142253
    HIV-1 inhibitor-10

    HIV Infection
    HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
  • HY-148043
    Schnurri-3 inhibitor-1

    Others Others
    Schnurri-3 inhibitor-1 is a potent schnurri-3 inhibitor which is an essential regulator of adult bone formation. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL with an AC50 value of 2.09 μM. Schnurri-3 inhibitor-1 can be used to research osteoporosis.
  • HY-146308
    HIV-1 inhibitor-26

    HIV Infection
    HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS.
  • HY-112614
    ATM Inhibitor-1

    ATM/ATR Cancer
    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.
  • HY-112373
    Aurora kinase inhibitor-3

    Aurora Kinase Others
    Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket.
  • HY-147750
    TDP1 Inhibitor-2

    Phosphodiesterase (PDE) Cancer Neurological Disease
    TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC50 of 3.5 μM.
  • HY-146127
    Grb2 SH2 domain inhibitor 1

    Others Others
    Grb2 SH2 domain inhibitor 1 is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
  • HY-128034
    PPIase-Parvulin inhibitor

    Others Cancer
    PPIase-Parvulin Inhibitor is a cell-permeable inhibitor of the PPIases Pin1 and Pin4 with IC50s of 1.5 and 1.0 µM, respectively.
  • HY-21141
    Cysteine protease inhibitor-2

    Cathepsin Cancer
    Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
  • HY-151163
    GLS1 Inhibitor-5

    Glutaminase Apoptosis Cancer
    GLS1 Inhibitor-5 (compound 24y) is an orally active selective glutaminase 1 (GLS1) inhibitor with an IC50 value of 68 nM. GLS1 Inhibitor-5 induces apoptosis and has anti-tumor activity.
  • HY-139376
    FGFR1 inhibitor-2

    FGFR Cancer
    FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer.
  • HY-119369
    FadD32 Inhibitor-1

    Bacterial Infection
    FadD32 Inhibitor-1 is a potent FadD32 inhibitor with anti-tubercular activity.
  • HY-150759
    HIV-1 inhibitor-45

    HIV Infection
    HIV-1 inhibitor-45 (compound IA-6) is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity.
  • HY-146089
    HIV-1 inhibitor-32

    HIV Infection
    HIV-1 inhibitor-32 (compound 3c) is a potent HIV-1 inhibitor with an IC50 value of 34 nM for WT HIV-1. HIV-1 inhibitor-32 can be used for researching AIDS.
  • HY-13329
    IRAK-1-4 Inhibitor I

    IRAK-1/4 inhibitor I

    IRAK Inflammation/Immunology
    IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
  • HY-18711A
    SCR-1481B1

    c-Met inhibitor 2

    c-Met/HGFR VEGFR Cancer
    SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
  • HY-139639
    MEK4 inhibitor-2

    MEK Cancer
    MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
  • HY-139638
    MEK4 inhibitor-1

    MEK Cancer
    MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
  • HY-139077
    SCD1 inhibitor-3

    Stearoyl-CoA Desaturase (SCD) Cancer Metabolic Disease
    SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer.
  • HY-147370
    HIV-1 inhibitor-46

    HIV Infection
    HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC50 value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS.
  • HY-128722
    HIV-1 inhibitor-3

    HIV Infection
    HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927.
  • HY-148042
    HIV-1 inhibitor-47

    HIV Infection
    HIV-1 inhibitor-47 is an inhibitor of HIV-1, and inhibits vif-dependent degradation of human APOBEC3G, with an IC50 value of 14.33 μM. HIV-1 inhibitor-47 also involves in derivatives of 1-(2-pyrimidinyl)piperazine synthesis, with potential antianxiety, antidepressant, and antipsychotic effect.
  • HY-147903
    HIV-1 inhibitor-42

    HIV Infection
    HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM.
  • HY-147552
    HIV-1 inhibitor-35

    HIV Infection
    HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent.
  • HY-147723
    HIV-1 inhibitor-39

    HIV Infection
    HIV-1 inhibitor-39 (compound 3c) is a potent HIV-1 inhibitor with an EC50 of >112.88 µM. HIV-1 inhibitor-39 shows anti-RT (HIV-1 reverse transcriptase) activities with an IC50 of 15.75 µM. HIV-1 inhibitor-39 shows cytotoxicity for MT-4 cells with an CC50 of 112.9 µM.
  • HY-150697
    HIV-1 inhibitor-44

    HIV Others
    HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM.
  • HY-136279
    TrxR inhibitor D9

    Apoptosis Cancer
    TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
  • HY-112843
    CNT2 inhibitor-1

    Others Others
    CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
  • HY-147553
    HIV-1 inhibitor-36

    HIV Infection
    HIV-1 inhibitor-36 (Compound 2) is a potent HIV-1. HIV-1 inhibitor-36 has the potential for further development as novel latency reversing agents.
  • HY-147555
    HIV-1 inhibitor-38

    HIV Infection
    HIV-1 inhibitor-38 (Compound 91) is a potent HIV-1. HIV-1 inhibitor-38 has the potential for further development as novel latency reversing agents.
  • HY-147554
    HIV-1 inhibitor-37

    HIV Infection
    HIV-1 inhibitor-37 (Compound 83) is a potent HIV-1. HIV-1 inhibitor-37 has the potential for further development as novel latency reversing agents.
  • HY-119372
    TDP1 Inhibitor-1

    Phosphodiesterase (PDE) Cancer
    TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM.
  • HY-147807
    HIV-1 inhibitor-40

    HIV Cytochrome P450 Infection
    HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity.
  • HY-132291
    HIV-1 inhibitor-8

    HIV Infection
    HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.
  • HY-115926
    BRD4 Inhibitor-16

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information.
  • HY-146091
    HIV-1 inhibitor-34

    HIV Infection
    HIV-1 inhibitor-34 (compound 5q) is a potent and selective HIV-1 inhibitor with an EC50 of 6.4 nM for HIV-1 and a CC50 of 16 μM in MT-4 cells. HIV-1 inhibitor-34 can be used for researching AIDS.
  • HY-148035
    Plm IV inhibitor-2

    Parasite Infection
    Plm IV inhibitor-2 (compound 3) is a potent digestive vacuole plasmepsins IV (Plm IV) inhibitor with IC50 values of 24 nM, 70 nM and 0.3 μM for Plm IV, II and I, respectively. Plm IV inhibitor-2 can be used to research malaria caused by Plasmodium parasites.
  • HY-122723
    GOT1 inhibitor-1

    Others Cancer
    GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
  • HY-147703
    Aurora kinase inhibitor-9

    Aurora Kinase Cancer
    Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity.
  • HY-146090
    HIV-1 inhibitor-33

    HIV Infection
    HIV-1 inhibitor-33 (compound 5n) is a potent and selective HIV-1 inhibitor with an EC50 of 8.6 nM for HIV-1 and a CC50 of 18 μM in MT-4 cells. HIV-1 inhibitor-33 can be used for researching AIDS.
  • HY-50865
    PDE-9 inhibitor

    Phosphodiesterase (PDE) Neurological Disease
    PDE-9 inhibitor is useful for neurodegenerative diseases.
  • HY-139092
    IL-4-inhibitor-1

    Interleukin Related Cancer Infection
    IL-4-inhibitor-1 (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 µM.
  • HY-146352
    HIV-1 inhibitor-28

    HIV Infection Inflammation/Immunology
    HIV-1 inhibitor-28 (compound 14j2) is a highly potent and selective HIV-1 inhibitor with an EC50 of 58 nM for WT HIV-1 strain and an IC50 of 3.37 μM for HIV-1 WT reverse transcription (RT). HIV-1 inhibitor-28 exhibits relatively low cytotoxicity in MT-4 cells (CC50 = 38.6 μM). HIV-1 inhibitor-28 can be used for researching AIDS.
  • HY-146339
    HIV-1 inhibitor-27

    HIV Infection Inflammation/Immunology
    HIV-1 inhibitor-27 (compound 5) is a potent HIV-1 inhibitor with IC50s of 16 μM, 0.5 μM and 0.39 μM for HIV-1 YU2, NL4-3 and 89.6 strain, respectively. HIV-1 inhibitor-27 has low cytotoxicity with a CC50 of 128 μM in TZM-bl cells. HIV-1 inhibitor-27 can be used for researching AIDS.
  • HY-147202
    BRD4 Inhibitor-24

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A).
  • HY-112390B
    Syk Inhibitor II dihydrochloride dihydrate

    Syk 5-HT Receptor Inflammation/Immunology
    Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect.
  • HY-150552
    JNK3 inhibitor-2

    JNK Discoidin Domain Receptor Cancer Inflammation/Immunology
    JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100, >100, 0.25 µM for JNK1, JNK2, JNK3, respectively. JNK3 inhibitor-2 shows DDR1 and EGFR (T790M, L858R) inhibition.
  • HY-136717
    FBPase-1 inhibitor-1

    FBPase Metabolic Disease
    FBPase-1 inhibitor-1 (compound 1) is a allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1).
  • HY-136270
    Gartisertib

    VX-803; M4344; ATR inhibitor 2

    ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
  • HY-136813
    Multitarget AD inhibitor-1

    Beta-secretase Amyloid-β Neurological Disease
    Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research.
  • HY-110243
    CAIX Inhibitor S4

    Carbonic Anhydrase Cancer
    CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.
  • HY-19990
    ALK kinase inhibitor-1

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK kinase inhibitor-1 is an anaplastic lymphoma kinase (ALK) inhibitor extracted from patent US20130261106A1 compound I-202.
  • HY-112681
    PKC-theta inhibitor

    PKC Others
    PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.
  • HY-146353
    HIV-1 inhibitor-29

    HIV Infection Inflammation/Immunology
    HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS.
  • HY-144122
    HIV-1 inhibitor-15

    HIV Infection
    HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability.
  • HY-112355
    Aurora kinase inhibitor-2

    Aurora Kinase Cancer
    Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.
  • HY-134851
    HIV-1 inhibitor-6

    HIV Infection
    HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to drugs targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM.
  • HY-151434
    GLS1 Inhibitor-6

    Glutaminase Apoptosis Cancer
    GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.
  • HY-150758
    NDM-1 inhibitor-3

    Bacterial Infection
    NDM-1 inhibitor-3 (Compound 89) is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor with a Ki of 4 μM.
  • HY-15183
    Collagen proline hydroxylase inhibitor

    Others Cancer
    Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor; useful for antifibroproliferative agents.
  • HY-144714
    HIV-1 inhibitor-18

    HIV Infection
    HIV-1 inhibitor-18 (compound II-13c) is a potent HIV-1 capsid inhibitor with an EC50 value of 5.14 μM for HIV-1 NL4-3. HIV-1 inhibitor-18 has certain cytotoxicity (MT-4 cells CC50 >9.51).
  • HY-144715
    HIV-1 inhibitor-17

    HIV Infection
    HIV-1 inhibitor-18 (compound V-25i) is a potent HIV-1 capsid inhibitor with an EC50 value of 2.57 μM for HIV-1 NL4-3. HIV-1 inhibitor-18 has certain cytotoxicity (MT-4 cells CC50 >8.55).
  • HY-146753
    HIV-1 inhibitor-20

    HIV Infection
    HIV-1 inhibitor-20 is a potent HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles.
  • HY-139631
    HIV-1 inhibitor-9

    HIV Infection
    HIV-1 inhibitor-9 is found to be potent inhibitor against the wild-type (WT) HIV-1 strain or multiple NNRTI-resistant strains at low nanomolar levels.
  • HY-124798
    Rheb inhibitor NR1

    mTOR Cancer Inflammation/Immunology Neurological Disease
    Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity.
    (Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
  • HY-144112
    HIV-1 inhibitor-13

    HIV Infection
    HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC50 values of 2.85-18.0 nM.
  • HY-147841
    HIV-1 inhibitor-41

    HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity.
  • HY-111429
    YAP/TAZ inhibitor-1

    YAP Cancer
    YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
  • HY-118355
    ALLM

    Calpain inhibitor II

    Proteasome Cathepsin Neurological Disease
    ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
  • HY-144123
    HIV-1 inhibitor-16

    HIV Infection
    HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity.
  • HY-112476
    PRL-3 Inhibitor I

    Phosphatase Cancer
    PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay.
  • HY-146746
    HIV-1 inhibitor-19

    HIV Infection
    HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
  • HY-146019
    HIV-1 inhibitor-24

    HIV Infection
    HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety.
  • HY-13972
    Mutant IDH1 inhibitor

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
  • HY-13985
    Nav1.7 inhibitor

    Sodium Channel Neurological Disease
    Nav1.7 inhibitor (compound II), a sulfonamide, is a potent Nav1.7 inhibitor. Nav1.7 inhibitor has the potential for a wide range of disorders, particularly pain.
  • HY-U00453
    Soluble epoxide hydrolase inhibitor

    Epoxide Hydrolase Metabolic Disease Cardiovascular Disease
    Soluble epoxide hydrolase inhibitor is an inhibitor of soluble epoxide hydrolase, and inhibits human soluble epoxide hydrolase (h-sEH) with pIC50 of 8.4, extracted from patent WO 2010096722 A1, example 57.
  • HY-112910
    Grp94 Inhibitor-1

    HSP Cancer Inflammation/Immunology
    Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
  • HY-144113
    HIV-1 inhibitor-14

    HIV Infection
    HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM.
  • HY-146018
    HIV-1 inhibitor-23

    HIV Infection
    HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability.
  • HY-150599
    HIV-1 inhibitor-43

    HIV DNA/RNA Synthesis Infection
    HIV-1 inhibitor-43 is a potent HIV-1 inhibitor with an EC50 of 21.3 nM, 6.2 nM, < 0.7 nM and < 0.7 nM for Y188L, K103N-Y181C, K103N and Y181C, respectively. HIV-1 inhibitor-43 can reduce HIV-1 RNA and protein p24 expression.
  • HY-112451
    cFMS Receptor Inhibitor II

    c-Fms Inflammation/Immunology
    cFMS Receptor Inhibitor II is a CSF1R kinase inhibitor. CSF-1 is a cytokine.
  • HY-103351
    Cathepsin G Inhibitor I

    Cathepsin Inflammation/Immunology
    Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.
  • HY-137471
    RBPJ Inhibitor-1

    RIN1

    Notch Cancer
    RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
  • HY-117491
    BRD4 Inhibitor-10

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM.
  • HY-P1111A
    Lyn peptide inhibitor TFA

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-146019A
    HIV-1 inhibitor-25

    HIV Infection
    HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1

    MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-19731
    SID 3712249

    MiR-544 inhibitor 1

    MicroRNA Apoptosis Cancer
    SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer.
  • HY-100734
    Histone Acetyltransferase Inhibitor II

    Histone Acetyltransferase Cancer
    Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
  • HY-136541
    YB-0158

    Wnt pathway inhibitor 2

    Wnt Apoptosis Cancer
    YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities.
  • HY-113951
    Prolyl Endopeptidase Inhibitor 1

    Boc-Pro-prolinal; (Boc)-Prolyl-prolinal; BPP

    Dipeptidyl Peptidase Neurological Disease
    Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a Ki value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.
  • HY-136149A
    Mpro inhibitor N3 hemihydrate

    SARS-CoV Virus Protease Infection
    Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively.
  • HY-146017
    HIV-1 inhibitor-22

    HIV Infection
    HIV-1 inhibitor-22 (compound 11a) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 3.63 μM for HIV-1 RT. HIV-1 inhibitor-22 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 0.304 μM and 0.201 μM, also has low cytotoxicity (CC50 > 227 μM)
  • HY-122862
    RAS inhibitor Abd-7

    Ras Cancer
    RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V.
  • HY-112392
    GSK-3 Inhibitor XIII

    GSK-3 Cancer
    GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM.
  • HY-112800
    cyt-PTPε Inhibitor-1

    Phosphatase Metabolic Disease
    cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
  • HY-147573
    BRD4 Inhibitor-23

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1).
  • HY-146015
    HIV-1 inhibitor-21

    HIV Infection
    HIV-1 inhibitor-21 (compound 9b) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 0.55 μM for HIV-1 RT. HIV-1 inhibitor-21 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 12.7 nM and 10.4 nM, and has relatively low cytotoxicity (MT-4 cells CC50 =10.2 μM).
  • HY-148034
    Plm IV inhibitor-1

    Others Infection
    Plm IV inhibitor-1 (compound 6) is a potent plasmepsin IV (Plm IV) inhibitor with IC50s of 4.1, 0.80, 0.25, 0.35 µM for Plm I, Plm II, Plm IV, Cat D, respectively.
  • HY-119375
    Syncytial Virus Inhibitor-1

    Bacterial Infection
    Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively.
  • HY-124366
    Slingshot inhibitor D3

    Others Cancer Infection
    Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2.
  • HY-14179
    PPQ-102

    CFTR inhibitor

    CFTR Others
    PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.
  • HY-116171
    (Rac)-Calpain Inhibitor XII

    Proteasome Neurological Disease Cardiovascular Disease
    (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
  • HY-15776
    HG-9-91-01

    SIK inhibitor 1

    Salt-inducible Kinase (SIK) Inflammation/Immunology
    HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.
  • HY-128888B
    (S,R)-WT IDH1 Inhibitor 2

    GSK321

    Isocitrate Dehydrogenase (IDH) Cancer
    (S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers.
  • HY-146365
    HIV-1 inhibitor-30

    HIV Infection Inflammation/Immunology
    HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS.
  • HY-115514A
    BRK inhibitor P21d hydrochloride

    Others Cancer
    BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
  • HY-15182
    Collagen proline hydroxylase inhibitor-1

    Others Cancer
    Collagen proline hydroxylase inhibitor-1 is an antifibroproliferative agents.
  • HY-104032
    Ac-CoA Synthase Inhibitor1

    RSV Infection Metabolic Disease
    Ac-CoA Synthase Inhibitor1 is a potent, reversible acetate-dependent acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 of 0.6 µM. Ac-CoA Synthase Inhibitor1 inhibits the respiratory syncytial virus (RSV).
  • HY-139606
    VCP/p97 inhibitor-1

    p97 Cancer
    VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS).
  • HY-123955
    Casein Kinase inhibitor A86

    Casein Kinase CDK Apoptosis Cancer
    Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
  • HY-13025
    HIV-1 integrase inhibitor

    HIV HIV Integrase Infection
    HIV-1 integrase inhibitor is uesful for anti-HIV.
  • HY-128729
    DNA2 inhibitor C5

    Others Cancer
    DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
  • HY-123905A
    LIN28 inhibitor LI71 enantiomer

    Others Cancer
    LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM.
  • HY-139720
    β-Secretase Inhibitor III

    Beta-secretase Neurological Disease
    β-Secretase Inhibitor III is an extremely selective BACE1 inhibitor (Ki = 0.13 nM).
  • HY-15222
    Menin-MLL inhibitor MI-2

    Epigenetic Reader Domain Apoptosis Cancer
    Menin-MLL inhibitor MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.
  • HY-14440
    MP7

    PDK1 inhibitor

    PDK-1 Cancer
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
  • HY-119935
    JAK3 covalent inhibitor-1

    JAK Inflammation/Immunology
    JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
  • HY-15167A
    Glyoxalase I inhibitor free base

    Others Cancer
    Glyoxalase I inhibitor (free base) is a potent Glyoxalase I (GLO1) inhibitor, candidate for anticancer agents.
  • HY-111378
    Casein Kinase II Inhibitor IV

    Casein Kinase Metabolic Disease
    Casein Kinase II Inhibitor IV is a potent, ATP-competitive of casein kinase II inhibitor with an IC50 of 9 nM. Casein Kinase II Inhibitor IV ia also a human keratinocytes (NHEK) differentiation inducer.
  • HY-147732
    sEH inhibitor-4

    Epoxide Hydrolase Inflammation/Immunology
    Intensive structural modification resulted in the identification of compound B15 as an effective sEH inhibitor with a value of 0.03 ± 0.01 nm, and the presence of soluble epoxide hydrolase (SEH) can reduce inflammation and pain.
  • HY-100983
    Protein kinase inhibitor H-7 dihydrochloride

    PKC Cancer
    Protein kinase inhibitor H-7 dihydrochloride is a potent PKC (protein kinase C) inhibitor. At 100 μM, Protein kinase inhibitor H-7 dihydrochloride completely inhibits both TPA (skin tumour promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase).
  • HY-128044
    Ftase inhibitor I

    B581

    Farnesyl Transferase Cancer
    Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras).
  • HY-126548
    β-Secretase Inhibitor I

    Beta-secretase Neurological Disease
    β-Secretase Inhibitor I is an extremely potent β-secretase inhibitor with reduced cardiovascular and liver toxicity.
  • HY-13060
    ACHP Hydrochloride

    IKK-2 inhibitor VIII

    IKK Inflammation/Immunology
    ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.
  • HY-P1045
    187-1, N-WASP inhibitor

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-15586
    L67

    DNA Ligase inhibitor

    DNA/RNA Synthesis Caspase Apoptosis Reactive Oxygen Species Cancer
    L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 (DNA Ligase Inhibitor) can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 (DNA Ligase Inhibitor) also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research.
  • HY-136736
    β-Secretase Inhibitor II

    Beta-secretase Neurological Disease
    β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total and IC50=2.5 μM for 1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.
  • HY-123954
    Casein Kinase inhibitor A51

    Casein Kinase CDK Apoptosis Cancer
    Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
  • HY-123772
    CDK5 inhibitor 20-223

    CDK Cancer
    CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
  • HY-112280
    CDK4/6/1 Inhibitor

    CDK Cancer
    CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
  • HY-P1382
    Rac1 Inhibitor W56

    Ras Cancer
    Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam.
  • HY-119934
    NaV1.7 inhibitor-1

    Sodium Channel Neurological Disease
    NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
  • HY-19991
    BMS-1

    PD-1/PD-L1 inhibitor 1

    PD-1/PD-L1 Apoptosis Cancer Inflammation/Immunology
    BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC50 between 6 and 100 nM).
  • HY-112164
    IACS-8968

    IDO/TDO inhibitor

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (IDO/TDO Inhibitor) is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-12276
    MALT1 inhibitor MI-2

    MALT1 Cancer
    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
  • HY-131900
    Protein kinase inhibitor H-7

    PKC Cancer
    Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC.
  • HY-117889
    PARP14 inhibitor H10

    PARP Apoptosis Cancer
    PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
  • HY-13949
    SRPIN340

    SRPK inhibitor

    SRPK Virus Protease Cancer
    SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
  • HY-123967
    RNF5 inhibitor inh-02

    Others Inflammation/Immunology
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
  • HY-145110
    IGF-1R inhibitor-2

    IGF-1R Cancer
    IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis.
  • HY-145946
    BRM/BRG1 ATP Inhibitor-2

    Epigenetic Reader Domain Cancer
    BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders.
  • HY-130493
    HPB

    HDAC6 inhibitor HPB

    HDAC Cancer
    HPB (HDAC6 inhibitor HPB) is a selective HDAC6 inhibitor with an IC50 of 31 nM. HPB exhibits >30-flod selectivity for HDAC6 over HDAC1.
  • HY-112462
    Cdk1/2 Inhibitor III

    CDK Cancer
    Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B.
  • HY-P1095
    Ivachtin

    Caspase-3 inhibitor VII

    Caspase Neurological Disease Cardiovascular Disease
    Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases.
  • HY-116716
    PIN1 inhibitor API-1

    MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-104022
    CHK1 inhibitor

    GDC-0575 analog

    Checkpoint Kinase (Chk) Cancer
    CHK1 inhibitor (GDC-0575 analog) is an inhibitor of CHK1.
  • HY-P1029
    MLCK inhibitor peptide 18

    Myosin CaMK Autophagy Others
    MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.
  • HY-10172
    IMD-0354

    IKK2 inhibitor V

    IKK Cancer
    IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
  • HY-15825
    IWP L6

    Porcn inhibitor III

    Porcupine Cancer
    IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
  • HY-19931
    COH29

    RNR inhibitor COH29

    DNA/RNA Synthesis Cancer
    COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
  • HY-P2477
    Human PD-L1 inhibitor IV

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1.
  • HY-123905
    LIN28 inhibitor LI71

    MicroRNA Cancer
    LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
  • HY-10133
    β-Secretase Inhibitor IV

    Beta-secretase Neurological Disease
    β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
  • HY-15155
    MLN0905

    PLK1 inhibitor

    Polo-like Kinase (PLK) Cancer
    MLN0905 is a potent PLK1 inhibitor, with an IC50 of 2 nM.
  • HY-124719
    hSMG-1 inhibitor 11j

    PI3K mTOR GSK-3 CDK Cancer
    hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
  • HY-129179
    Lisaftoclax

    APG-2575; Bcl-2/Bcl-xl inhibitor 1

    Bcl-2 Family Cancer
    Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
  • HY-P2564
    Human PD-L1 inhibitor III

    PD-1/PD-L1 Cancer Inflammation/Immunology
    Human PD-L1 inhibitor III is a human PD-L1 inhibitor.
  • HY-15339
    CVT-313

    Cdk2 inhibitor III

    CDK Cancer
    CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
  • HY-13487
    USP7/USP47 inhibitor

    Deubiquitinase Cancer
    USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
  • HY-12220
    MM-102

    HMTase inhibitor IX

    Histone Methyltransferase Cancer
    MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor, achieves IC50= 2.4 nM with an estimated Ki< 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
  • HY-W404002
    BR102910

    Prolyl Endopeptidase (PREP) Metabolic Disease
    BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
  • HY-147734
    Calpain Inhibitor-2

    Others Cancer
    Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
  • HY-P1045A
    187-1, N-WASP inhibitor TFA

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-18236
    MDL-28170

    Calpain inhibitor III

    Proteasome Inflammation/Immunology Neurological Disease
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.
  • HY-111378A
    Casein Kinase II Inhibitor IV Hydrochloride

    Casein Kinase Others
    Casein Kinase II Inhibitor IV Hydrochloride is a small-molecule inducer of epidermal keratinocyte differentiation.
  • HY-124760
    hSMG-1 inhibitor 11e

    mTOR PI3K CDK Cancer
    hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM).
  • HY-P2470
    Human PD-L1 inhibitor II

    PD-1/PD-L1 Cancer
    Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.
  • HY-14971
    (E)-Akt inhibitor-IV

    (E)-AKTIV

    Akt Cancer
    (E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic.
  • HY-P1382A
    Rac1 Inhibitor W56 TFA

    Ras Cancer
    Rac1 Inhibitor W56 TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 TFA inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam.
  • HY-P2478
    Human PD-L1 inhibitor V

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor V, a human PD-1 protein binding peptide with a Kd value of 3.32 μM. Human PD-L1 inhibitor V inhibit the interaction of hPD-1/hPD-L1.
  • HY-15610
    GDC-0623

    RG 7421; MEK inhibitor 1

    MEK Apoptosis Cancer
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
  • HY-141476
    PI3K/mTOR Inhibitor-3

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity.
  • HY-112915
    Eg5 Inhibitor V, trans-24

    Kinesin Cancer
    Eg5 Inhibitor V, trans-24 is a potent and specific kinesin Eg5 inhibitor with an IC50 of 0.65 μM, and can be used in the research of cancer.
  • HY-147613
    PI3K/mTOR Inhibitor-6

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-6 displays better stability in artificial gastric fluids than gedatolisib. PI3K/mTOR Inhibitor-6 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-6 has the potential for the research of cancer diseases.
  • HY-147724
    Microtubule inhibitor 3

    Microtubule/Tubulin Cancer
    Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
  • HY-146203
    FAK inhibitor 6

    FAK Cancer
    Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
  • HY-147728
    Microtubule inhibitor 7

    Microtubule/Tubulin Cancer
    Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
  • HY-112147
    IDO1 and HDAC1 Inhibitor

    Indoleamine 2,3-Dioxygenase (IDO) HDAC Cancer
    IDO1 and HDAC1 Inhibitor (Compound 10) is a dual IDO1 and HDAC1 inhibitor with IC50s of 69.0 nM and 66.5 nM, respectively.
  • HY-147614
    PI3K/mTOR Inhibitor-7

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-7 shows 4.7-fold higher potency than the positive control gedatolisib (0.3 vs. 1.4 μM, IC50 values). PI3K/mTOR Inhibitor-7 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-7 has the potential for the research of cancer diseases.
  • HY-125257
    SHP2 inhibitor LY6

    LY6

    Phosphatase Cancer
    SHP2 inhibitor LY6 (LY6) is potent and selective inhibitor of SHP2, with an IC50 of 9.8 µM. SHP2 inhibitor LY6 can inhibits SHP2-mediated cell signaling and proliferation.
  • HY-U00410
    PDE4 inhibitor intermediate 1

    Others Others
    PDE4 inhibitor intermediate 1 is an intermediate for PDE4 inhibitor synthesis.
  • HY-13319
    JNK-IN-8

    JNK inhibitor XVI

    JNK Cancer
    JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.
  • HY-100110
    KNK437

    Heat Shock Protein inhibitor I

    HSP Cancer
    KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
  • HY-P0299
    LSKL, Inhibitor of Thrombospondin (TSP-1)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.
  • HY-124718
    p32 Inhibitor M36

    M36

    PKC Cancer
    p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
  • HY-15617
    JNK-IN-7

    JNK inhibitor

    JNK Cancer
    JNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.
  • HY-146016
    PI3K/mTOR Inhibitor-5

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-5 (compound 19a) is a potent and dual PI3K and mTOR inhibitor, with IC50 values of 86.9 nM and 14.6 nM, respectively.
  • HY-101462
    RAD51 Inhibitor B02

    B02

    RAD51 Apoptosis Cancer
    RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM.
  • HY-112420
    EGFR/ErbB-2/ErbB-4 inhibitor-2

    EGFR Cancer
    EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.
  • HY-103002
    SU5408

    VEGFR2 Kinase inhibitor I

    VEGFR Cardiovascular Disease
    SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
  • HY-124653
    HSP27 inhibitor J2

    J2

    HSP Cancer
    HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
  • HY-146200
    PI3K/mTOR Inhibitor-8

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase.
  • HY-107412
    Proteasome inhibitor IX

    PS-IX; AM114

    Proteasome Cancer
    Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
  • HY-112401
    p38 MAP Kinase Inhibitor IV

    p38 MAPK Inflammation/Immunology
    p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively.
  • HY-10355
    AKT inhibitor VIII

    AKTi-1/2

    Akt Apoptosis Cancer Metabolic Disease
    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
  • HY-144189
    PRMT5-IN-18

    Histone Methyltransferase Cancer
    PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5, such as cancer.
  • HY-13946
    BML-277

    Chk2 inhibitor II

    Checkpoint Kinase (Chk) Apoptosis Cancer
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
  • HY-122720
    SEC inhibitor KL-1

    KL-1

    Others Cancer
    SEC inhibitor KL-1 (KL-1), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 3.48 μM.
  • HY-123972
    SEC inhibitor KL-2

    KL-2

    Others Cancer
    SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM.
  • HY-P2478A
    Human PD-L1 inhibitor V TFA

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor V TFA, a human PD-1 protein binding peptide with a Kd value of 3.32 μM. Human PD-L1 inhibitor V TFA inhibit the interaction of hPD-1/hPD-L1.
  • HY-147653
    Integrase-LEDGF/p75 allosteric inhibitor 1

    HIV Integrase Infection
    Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432.
  • HY-124861
    Malic enzyme inhibitor ME1

    ME1

    Others Cancer Metabolic Disease
    Malic enzyme inhibitor ME1 (ME1; compound 1) is a potent inhibitor of Malic enzyme (ME1) with an IC50 of 0.15 μM.
  • HY-15881
    TCS JNK 5a

    JNK inhibitor IX

    JNK Apoptosis Cancer
    TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
  • HY-103440
    EGFR/ErbB-2/ErbB-4 inhibitor-3

    EGFR Cancer
    EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively.
  • HY-15526
    PSI-697

    P-Selectin inhibitor

    Others Cancer
    PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM.
  • HY-120145
    MST-312

    Telomerase inhibitor IX

    Telomerase Cancer
    MST-312 is a telomerase inhibitor. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 can be used for the research of cancer, such as multiple myeloma (MM).
  • HY-145231
    FGFR2-IN-2

    FGFR Cancer
    FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor with IC50s of 389, 29, and 758 nM for FGFR1, FGFR2, and FGFR3, respectively.
  • HY-13033
    CDK-IN-2

    CDK inhibitor II

    CDK Cancer
    CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
  • HY-P0299A
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
  • HY-16990
    Ac-YVAD-cmk

    Caspase-1 inhibitor II

    Caspase Inflammation/Immunology
    Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases.
  • HY-14445
    FK 3311

    COX-2 inhibitor V

    COX Inflammation/Immunology
    FK 3311 (COX-2 Inhibitor V) is a selective inhibitor of COX-2 with antiinflammatory agent.
  • HY-19707
    4μ8C

    IRE1 inhibitor III

    IRE1 Metabolic Disease
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
  • HY-70027A
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.
  • HY-N10227
    Geodin

    PAI-1 Antibiotic Infection Inflammation/Immunology
    Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1).
  • HY-10324
    D4476

    Casein Kinase I inhibitor

    Casein Kinase Autophagy Apoptosis Cancer
    D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
  • HY-W096600
    2F-Peracetyl-Fucose

    1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos

    Others Cancer
    2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) acts as a potent fucosyltransferase (FUT) inhibitor.
  • HY-15282
    E-64

    Proteinase inhibitor E 64

    Cathepsin Autophagy Bacterial Inflammation/Immunology Cancer
    E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
  • HY-147285
    PI3K/mTOR Inhibitor-9

    mTOR PI3K Neurological Disease
    PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively.
  • HY-15609
    AZD-3463

    ALK/IGF1R inhibitor

    Anaplastic lymphoma kinase (ALK) IGF-1R Autophagy Apoptosis Cancer Endocrinology
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.
  • HY-112544
    IK1 inhibitor PA-6

    PA-6

    Potassium Channel Cardiovascular Disease
    IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
  • HY-12220A
    MM-102 TFA

    HMTase inhibitor IX TFA

    Histone Methyltransferase Cancer
    MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
  • HY-107598
    JNK Inhibitor VIII

    TCS JNK 6o

    JNK Cancer
    JNK Inhibitor VIII (TCS JNK 6o) is a c-Jun N-terminal kinases (JNK-1, -2, and -3) inhibitor with Ki values of 2 nM, 4 nM, 52 nM, respectively, and has IC50 values of 45 nM and 160 nM for JNK-1 and -2, respectively.
  • HY-111508
    PI3K/mTOR Inhibitor-2

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
  • HY-112602
    PI3K/mTOR Inhibitor-1

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.
  • HY-142834
    RORγt/DHODH-IN-2

    ROR Dihydroorotate Dehydrogenase Inflammation/Immunology
    RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research.
  • HY-137552
    MKI-1

    MASTL Kinase inhibitor-1

    Others Cancer
    MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
  • HY-147250A
    FGFR2-IN-3 hydrochloride

    EGFR Cancer
    FGFR2-IN-3 hydrochloride is an orally active selective inhibitor of FGFR2.
  • HY-147250
    FGFR2-IN-3

    EGFR Cancer
    FGFR2-IN-3 is an orally active selective inhibitor of FGFR2.
  • HY-17602
    Amcasertib

    BBI503

    Others Cancer
    Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitory activity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
  • HY-117370
    USP25/28 inhibitor AZ1

    AZ1

    Deubiquitinase Cancer
    USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
  • HY-144708
    Axl-IN-4

    TAM Receptor Cancer
    Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC50 of 28.8 μM.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-15887
    MG 149

    Tip60 HAT inhibitor

    Histone Acetyltransferase Epigenetic Reader Domain Apoptosis Cancer
    MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM).
  • HY-101799
    NCGC00244536

    KDM4B inhibitor B3

    Histone Demethylase Cancer
    NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
  • HY-70027
    p53 and MDM2 proteins-interaction-inhibitor (chiral)

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
  • HY-B0331
    Enalapril

    MK-421

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease Cancer
    Enalapril (MK-421) is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research.
  • HY-B0331B
    Enalapril sodium

    MK-421 sodium

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalapril (MK-421) sodium is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research.
  • HY-70028
    p53 and MDM2 proteins-interaction-inhibitor (racemic)

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    p53 and MDM2 proteins-interaction-inhibitor (racemic) (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.
  • HY-142706
    MAO A/HDAC-IN-1

    Monoamine Oxidase HDAC Cancer
    MAO A/HDAC-IN-1 is a dual inhibitor of monoamine oxidase A (MAO A) and HDAC. MAO A/HDAC-IN-1 can be used for glioma research.
  • HY-13671
    LW6

    HIF-1α inhibitor; LW8

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
  • HY-18964
    MG-101

    Calpain inhibitor I; Ac-LLnL-CHO; ALLN

    Proteasome Apoptosis Cancer
    MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
  • HY-151197
    HIV protease-IN-1

    HIV Protease Infection
    HIV protease-IN-1 (compound 1·succinate) is a potent HIV protease non-peptidic inhibitor, can be used to research AIDS.
  • HY-110156
    YZ9

    Others Cancer
    Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM.
  • HY-112164B
    IACS-8968 S-enantiomer

    IDO/TDO inhibitor (S-enantiomer)

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (S-enantiomer) is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-112164A
    IACS-8968 R-enantiomer

    IDO/TDO inhibitor (R-enantiomer)

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (R-enantiomer) is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-16661
    Skp2 Inhibitor C1

    SKPin C1

    E1/E2/E3 Enzyme Cancer
    Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
  • HY-12299
    WH-4-023

    Dual LCK/SRC inhibitor

    Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
  • HY-P1028A
    Hexa-D-arginine TFA

    Furin inhibitor II TFA

    Bacterial Infection
    Hexa-D-arginine TFA (Furin Inhibitor II TFA) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine TFA blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo.
  • HY-12652
    AZD3147

    mTOR Cancer
    AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K.
  • HY-10038
    A 922500

    DGAT-1 inhibitor 4a

    Acyltransferase Metabolic Disease
    A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
  • HY-P1290
    PKA Inhibitor Fragment (6-22) amide

    PKI-(6-22)-amide

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-10721
    PF-AKT400

    AKT protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • HY-126200
    Fenpropidin

    Fungal Infection
    Fenpropidin is a sterol biosynthesis inhibitor fungicide.
  • HY-147229
    GDC-6036-NH

    Ras Cancer
    GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research.
  • HY-16214
    FX-11

    LDHA inhibitor FX11

    Lactate Dehydrogenase Pyruvate Kinase Apoptosis Reactive Oxygen Species Cancer
    FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) specific inhibitor, with a Ki of 8 μM. FX-11 can effectively activate PKM2 (pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.
  • HY-117997
    UMB-32

    Epigenetic Reader Domain Cancer
    UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor.
  • HY-15480
    NSC 42834

    JAK2 inhibitor V; Z3

    JAK Cancer
    NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
  • HY-110077
    API-1

    Akt Apoptosis Cancer
    API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL).
  • HY-119823
    PGP-4008

    P-glycoprotein Cancer
    PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin.
  • HY-10035
    TTA-P2

    T-Type calcium channel inhibitor

    Calcium Channel Neurological Disease
    TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
  • HY-15813
    FIIN-1

    FGFR irreversible inhibitor-1

    FGFR Cancer
    FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.
  • HY-122098
    Diaplasinin

    PAI-749

    PAI-1 Cardiovascular Disease
    Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy.
  • HY-15425
    PF-543

    Sphingosine Kinase 1 inhibitor II

    SphK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.
  • HY-15425B
    PF-543 hydrochloride

    Sphingosine Kinase 1 inhibitor II hydrochloride

    SphK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
  • HY-150680
    SARS-CoV-2 nsp14-IN-1

    SARS-CoV Histone Methyltransferase DNA Methyltransferase Infection
    SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases.
  • HY-125344
    Fusarisetin A

    Endogenous Metabolite Infection
    Fusarisetin A, a pentacyclic fungal metabolite, is an acinar morphogenesis inhibitor.
  • HY-46568
    CDK7/12-IN-1

    CDK Cancer
    CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.
  • HY-119857
    AGK7

    SIRT2 inhibitor,Inactive Control

    Sirtuin Neurological Disease
    AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease.
  • HY-147258
    Culmerciclib

    Cyclin G-associated Kinase (GAK) Cancer
    Culmerciclib is a cyclin dependent kinase (CDK) inhibitor, and has antineoplastic activity.
  • HY-114903
    (E/Z)-BIO-acetoxime

    GSK-​3 inhibitor X

    GSK-3 CDK Cancer Metabolic Disease Neurological Disease
    (E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM).
  • HY-18007
    ALW-II-41-27

    Eph receptor tyrosine kinase inhibitor

    Ephrin Receptor Cancer
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
  • HY-19992
    3-Bromopyruvic acid

    Bromopyruvic acid; Hexokinase II inhibitor II, 3-BP

    Hexokinase Apoptosis Autophagy Cancer
    3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.
  • HY-15508
    JANEX-1

    WHI-P131; Jak3 inhibitor I

    JAK Cancer
    JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
  • HY-125666
    Agistatin B

    Others Infection
    Agistatin B, isolated from fungus, is a mycotoxin. Agistatin B inhibits cholesterol synthesis.
  • HY-144700
    Antileishmanial agent-3

    Parasite Infection
    Antileishmanial agent-3 (Compound 13) is a promising growth inhibitor of Leishmania major.
  • HY-107613
    R 59-022

    DKGI-I; Diacylglycerol kinase inhibitor I

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-13057
    O6BTG-octylglucoside

    Glucose-conjugated MGMT inhibitor

    DNA Methyltransferase Cancer
    O6BTG-octylglucoside is a potent O 6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
  • HY-100960
    Dioctanoylglycol

    Ethylene glycol dicaprylate; Ethylene glycol dioctanoate; Ethylenedioctanoate

    Others Cardiovascular Disease
    Dioctanoylglycol (Ethylene glycol dicaprylate), a diacylglycerol analog, is a diacylglycerol kinase (DGK) inhibitor (Ki of 58 μM).
  • HY-142922
    BCR-ABL-IN-4

    Bcr-Abl Cancer
    BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11).
  • HY-117043
    GRL0617

    Deubiquitinase SARS-CoV Infection
    GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome.
  • HY-N10234
    Phenylpyropene A

    Acyltransferase Infection
    Phenylpyropene A, a fungal metabolite, is a potent acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor with an IC50 of 0.8 μM.
  • HY-146752
    α-Amylase-IN-1

    Others Others
    α-Amylase-IN-1 is a potent α-amylase inhibitor with an IC50 of 4.46 μM.
  • HY-D1084
    7-Hydroxy-4-methylcoumarin-3-acetic acid

    Others Others
    7-Hydroxy-4-methylcoumarin-3-acetic acid is a growth inhibitor of root.
  • HY-50900
    gamma-Secretase Modulators

    Amyloid-β production inhibitor; γ-Secretase Modulators

    Amyloid-β Neurological Disease
    gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor.
  • HY-113542
    Blasticidin A

    (+)-Blasticidin A

    Bacterial Antibiotic Infection
    Blasticidin A ((+)-Blasticidin A) is an inhibitor of Aflatoxin production by Aspergillus parasiticus. Blasticidin A almost completely inhibits Aflatoxin production at 0.5 μM. Blasticidin A is a potent antibiotic produced by Streptomyces, inhibits Aflatoxin production without strong growth inhibition toward Aflatoxin-producing fungi.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-101947
    SMI-16a

    PIM1/2 Kinase inhibitor VI

    Pim Cancer
    SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
  • HY-B0397
    Dichlorphenamide

    Diclofenamide

    Carbonic Anhydrase Neurological Disease
    Dichlorphenamide (Diclofenamide) is an orally active, specific, carbonic anhydrase inhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research.
  • HY-B0397A
    Dichlorphenamide disodium

    Diclofenamide disodium

    Carbonic Anhydrase Neurological Disease
    Dichlorphenamide (Diclofenamide) disodium is an orally active, specific, carbonic anhydrase inhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research.
  • HY-P1290A
    PKA Inhibitor Fragment (6-22) amide TFA

    PKI-(6-22)-amide TFA

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-14394
    TBB

    NSC 231634; Casein Kinase II inhibitor I

    Casein Kinase Cancer
    TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
  • HY-109108A
    Valemetostat tosylate

    DS-3201 tosylate

    Histone Methyltransferase Cancer
    Valemetostat tosylate (DS-3201 tosylate), a first-in-class EZH1/2 dual inhibitor. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
  • HY-N10198
    Acremonidin A

    Endogenous Metabolite Calmodulin Cardiovascular Disease
    Acremonidin A is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremonidin A binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 19.40 nM.
  • HY-117678
    TG-2-IN-1

    Glutaminase Others
    TG-2-IN-1 (Compound D003) is a transglutaminase-2 (TGM-2) inhibitor. TG-2-IN-1 can be used for the research of myopia.
  • HY-127026A
    Quinaprilat hydrate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator.
  • HY-N10199
    Acremoxanthone C

    Endogenous Metabolite Calmodulin Cardiovascular Disease
    Acremoxanthone C is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremoxanthone C binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 18.25 nM.
  • HY-143431
    Cdc7-IN-17

    CDK Cancer
    Cdc7-IN-17 is a potent CDC7 inhibitor with an IC50 of <10 μM, extracted from patent WO2018217439A1. Cdc7-IN-17 can be used for cancer research.
  • HY-127026
    Quinaprilat

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat is an orally active non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat acts as anti-hypertensive agent and vasodilator.
  • HY-150022
    GRK5-IN-4

    CCG-265328

    G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research.
  • HY-15425A
    PF-543 Citrate

    Sphingosine Kinase 1 inhibitor II Citrate

    SphK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
  • HY-144690
    D5261

    Trk Receptor Cancer
    D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
  • HY-150691
    SARS 3CLpro-IN-1

    SARS-CoV Cancer
    SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomer of the octahydroisochromene scaffold, directs the P1 site imidazole.
  • HY-P0081
    Bax inhibitor peptide V5

    BIP-V5; BAX Inhibiting Peptide V5

    Bcl-2 Family Cancer
    Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
  • HY-145046
    SOS1-IN-3

    Ras Cancer
    SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1).
  • HY-108356
    NS3694

    Apoptosis Cancer
    NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation.
  • HY-146741
    SDR-04

    Epigenetic Reader Domain Cancer
    SDR-04 is BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.
  • HY-N10232
    Agistatin E

    Others Infection
    Agistatin E is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.
  • HY-N10231
    Agistatin D

    Others Infection Inflammation/Immunology
    Agistatin D is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.
  • HY-149015
    FTase-IN-1

    Farnesyl Transferase Cancer
    FTase-IN-1 (compound 17a) is a potent and specific inhibitor of fanesyl transferase (FTase) with an IC50 of 0.35 μM. FTase-IN-1 displays cytotoxicity potential and antitumor activity.
  • HY-10704
    PTP1B-IN-1

    PTP1B inhibitor

    Phosphatase Metabolic Disease
    PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
  • HY-W376701
    Guanadrel

    Adrenergic Receptor Cardiovascular Disease
    Guanadrel is an orally active postganglionic adrenergic inhibitor of spiroketal. Guanadre can be used in anti-hypertensive studies.
  • HY-50730
    Asparagusic acid

    Parasite Infection
    Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
  • HY-16776A
    (2S,5S)-Censavudine

    (2S,5S)-OBP-601; (2S,5S)-BMS-986001

    HIV Infection
    (2S,5S)-Censavudine ((2S,5S)-OBP-601) is the (2S,5S)-enantiomer of Censavudine. Censavudine, a nucleoside reverse transcriptase inhibitor, is a potent HIV inhibitor.
  • HY-150551
    COX-2-IN-27

    COX Inflammation/Immunology
    COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC50 values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity.
  • HY-B0312
    Dipyridamole

    Phosphodiesterase (PDE) Cardiovascular Disease
    Dipyridamole is an antiplatelet agent used in secondary prophylaxis against stroke.
    . Dipyridamole also can induce cancer cell-specific apoptosis as a phosphodiesterase (PDE) inhibitor.
    .
  • HY-150510
    MS8511

    Histone Methyltransferase Cancer Neurological Disease
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
  • HY-116530
    9-Cyclopentyladenine monomethanesulfonate

    9-CP-Ade mesylate

    Adenylate Cyclase Neurological Disease Others
    9-Cyclopentyladenine monomethylsulfonate (9-CP-Ade mesylate) is a stable non-competitive adenylate cyclase inhibitor with cell permeable properties.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-150577
    HDAC-IN-45

    HDAC Cancer
    HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
  • HY-150625
    SARS-CoV-2 nsp13-IN-4

    SARS-CoV Infection
    SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective nsp13 helicase small-molecule inhibitor and inhibit the ssDNA+ ATPase activity of nsp13 with an IC50 value of 57 μM. SARS-CoV-2 nsp13-IN-4 is druglike molecule with molecular weight of less than 450Da and can provide a broad-spectrum antiviral effect.
  • HY-144681
    LY3372689

    Others Neurological Disease
    LY3372689 is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.
  • HY-10371
    Pim1/AKK1-IN-1

    LKB1/AAK1 dual inhibitor

    Pim Cancer
    Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
  • HY-150766
    KPC-2-IN-1

    Bacterial Infection
    KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics.
  • HY-143475
    POP-IN-2

    Prolyl Endopeptidase (PREP) Cancer Neurological Disease
    POP-IN-2 (Compound 7k) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 6 nM. POP-IN-2 can be used for studying neurodegenerative diseases and cancer.
  • HY-143474
    Y-29794

    Prolyl Endopeptidase (PREP) Cancer Neurological Disease
    Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer.
  • HY-142687
    SGK1-IN-4

    SGK Inflammation/Immunology
    SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research.
  • HY-108607
    PACOCF3

    Palmityltrifluoromet​hylketone

    Phospholipase Inflammation/Immunology
    PACOCF3 (Palmityltrifluoromet​hylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca 2+ signaling in renal tubular cells.
  • HY-147216
    AXKO-0046

    Others Cancer
    AXKO-0046 is an indole derivative and small-molecule LDHB selective inhibitor.
  • HY-143471
    PLK1/BRD4-IN-1

    Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Cancer
    PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity.
  • HY-108623
    Atizoram

    CP-80,633

    Phosphodiesterase (PDE) Inflammation/Immunology
    Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice.
  • HY-101144
    RSM-932A

    TCD-717

    Others Cancer
    RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
  • HY-150644
    S07-2010

    Others Cancer
    S07-2010 is a potent pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3, AKR1C4, AKR1C1 and AKR1C2, respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells.
  • HY-101776
    Desmethyl-VS-5584

    Desmethyl-SB2343

    mTOR PI3K Cancer
    Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure.
  • HY-150737
    MI-1851

    SARS-CoV Infection
    MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity.
  • HY-119046
    SNX-0723

    HSP Parasite Infection
    SNX-0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX-0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX-0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM.
  • HY-136521
    AZ13824374

    Epigenetic Reader Domain Cancer
    AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively.
  • HY-11012
    TDZD-8

    GSK-3β inhibitor I; NP 01139

    GSK-3 Cancer
    TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
  • HY-144882
    (R)-HH2853

    Histone Methyltransferase Cancer Inflammation/Immunology
    (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201).
  • HY-144264
    hCAII-IN-6

    Carbonic Anhydrase Endocrinology
    hCAII-IN-6 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor with a Ki of 4.4 nM. hCAII-IN-6 also inhibits other hCAs isoforms I, IV and IX, with Ki values of 9.2 nM, 480.2 nM and 14.7 nM, respectively. hCAII-IN-6 can be used for glaucoma research.
  • HY-103663A
    MAK683 hydrochloride

    Histone Methyltransferase Cancer
    MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
  • HY-150573
    CDK2-IN-12

    CDK Carbonic Anhydrase Cancer
    CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity.
  • HY-108444
    (Z)-FeCP-oxindole

    VEGFR Cancer
    (Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM.
  • HY-147289
    NSC 698600

    Histone Acetyltransferase Cancer
    NSC 698600 is a potent PCAF inhibitor, with IC50 of 6.51 µM (PCAF/H31-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells.
  • HY-147288
    NSC 694621

    Histone Acetyltransferase Cancer
    NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 µM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells.
  • HY-147930
    ACC1/2-IN-1

    Acetyl-CoA Carboxylase Cancer
    ACC1/2-IN-1 (compound 4s) is a potent ACC1/2 inhibitor with IC50 values of 98.06 and 29.43 nM for ACC1 and ACC2, respectively. ACC1/2-IN-1 can be used for cancer research.
  • HY-145159
    SHP2 protein degrader-1

    PROTACs Phosphatase Apoptosis Cancer
    SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases.
  • HY-143872
    Bcl-2-IN-4

    Bcl-2 Family Cancer
    Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2).
  • HY-144031S
    Tyk2-IN-8

    JAK Inflammation/Immunology
    Tyk2-IN-8 (Compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease.
  • HY-144824
    Monoamine oxidase/Aromatase-IN-1

    Monoamine Oxidase Aromatase Cancer Neurological Disease
    Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a highly potent monoamine oxidase (MAO) and aromatase dual inhibitor with IC50s of 39 nM and 31 nM for MAO-B and aromatase, respectively. Monoamine oxidase/Aromatase-IN-1 can be used for researching neurological disorder and breast cancer.
  • HY-142031
    4-Piperidinecarboxamide

    Bacterial Infection
    4-Piperidinecarboxamide is a mycobacterial aspartyl-tRNA synthetase (AspS) inhibitor. 4-Piperidinecarboxamide is a promising anti-tuberculosis (TB) agent.
  • HY-113534
    MV1

    IAP Apoptosis Cancer
    MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
  • HY-147932
    ACC1/2-IN-2

    Acetyl-CoA Carboxylase Cancer
    ACC1/2-IN-2 (compound PF-3) is a potent ACC1/2 inhibitor with IC50 values of 22 and 48 nM for ACC1 and ACC2, respectively. ACC1/2-IN-2 has antiproliferation activity and can be used for cancer research.
  • HY-145435
    SARS-CoV-2-IN-12

    SARS-CoV Infection
    SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19.
  • HY-116804
    ZLD1039

    Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
  • HY-P9902
    Pembrolizumab

    MK-3475; Lambrolizumab; Keytruda

    PD-1/PD-L1 Cancer
    Pembrolizumab (MK-3475) is a humanized IgG4 antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
  • HY-149006
    CK156

    DAPK Inflammation/Immunology Cancer
    CK156 is a highly selective death-associated protein kinase (DAPK) inhibitor with IC50s of 182 nM,34 μM, and 39 μM in the DRAK1 NanoBRET assay for DRAK1, CK2a1, and CK2a2, respectively. CK156 can be used for the research of autoimmune and inflammatory diseases.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-13645
    Henatinib

    VEGFR c-Kit PDGFR Cancer
    Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs).
  • HY-121827
    LH21

    Cannabinoid Receptor Metabolic Disease
    LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats. , and displays efficacy as a feeding inhibitor.
  • HY-143886
    AD011

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    AD011 is a dual inhibitor of cACE/NEP. AD011 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD011 has the potential for providing the potent antihypertensive and cardioprotective benefits.
  • HY-143888
    AD013

    Angiotensin-converting Enzyme (ACE) Others
    AD013 is a dual inhibitor of cACE/NEP. AD013 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD013 has the potential for providing the potent antihypertensive and cardioprotective benefits.
  • HY-143887
    AD012

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    AD012 is a dual inhibitor of cACE/NEP. AD012 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD012 has the potential for providing the potent antihypertensive and cardioprotective benefits.
  • HY-150560
    α-Glucosidase-IN-11

    Glucosidase Metabolic Disease
    α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels.
  • HY-N6794
    10Z-Hymenialdisine

    (Z)-Hymenialdisine; Hymenialdisine

    AMPK VEGFR PDGFR Cancer
    10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.
  • HY-146137
    Transthyretin-IN-1

    Others Neurological Disease
    Transthyretin-IN-1 (Compound 1d) is a transthyretin (TTR) fibril formation inhibitor. Transthyretin-IN-1 can be used for Alzheimer’s disease research.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-144032
    Tyk2-IN-9

    JAK Inflammation/Immunology
    Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease.
  • HY-103263
    PSB-06126

    Phosphatase Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
    PSB-06126 is a selective nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with the Ki values of 0.33 μM for rat NTPDase 1, 19.1 μM for NTPDase 2 and 2.22 μM for NTPDase 3, respectively. PSB-06126 acts on human NTPDase 3 with an IC50 value of 7.76 μM and a Ki value of 4.39 μM.
  • HY-146297
    Xanthine oxidoreductase-IN-2

    Xanthine Oxidase Metabolic Disease
    Xanthine oxidoreductase-IN-2 (Compound IVa) is a xanthine oxidoreductase (XOR) inhibitor with the IC50 of 7.2 nM. Xanthine oxidoreductase-IN-2 shows hypouricemic effects in mice.
  • HY-145809
    FASN-IN-5

    Fatty Acid Synthase (FASN) Cancer Inflammation/Immunology Metabolic Disease
    FASN-IN-5 (example 11), a FASN inhibitor, can be used for the research of TH17- or CSF1 -mediated disease or disorder such as cancer, immunological disorders, and obesity.
  • HY-B1287
    Citalopram hydrobromide

    (±)-Citalopram hydrobromide; Lu 10-171

    Serotonin Transporter Autophagy Neurological Disease Cancer
    Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
  • HY-144087
    TYK2-IN-11

    JAK Inflammation/Immunology
    TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease.
  • HY-B1433
    Perindoprilat

    S 9780

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research.
  • HY-143258
    CDK4/6-IN-8

    CDK Cancer
    CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC50 values of 5.01 nM and 3.97 nM, respectively.
  • HY-15879
    LB42708

    Farnesyl Transferase Apoptosis Inflammation/Immunology
    LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively.
  • HY-103358
    KF38789

    Others Inflammation/Immunology
    KF38789 is a selective inhibitor of P-selectin-PSGL-1 binding. KF38789 inhibits the binding of U937 cells to immobilized P-selectin immunoglobulin G chimeric protein (P-selectin-Ig) with an IC50 value of 1.97 μM.
  • HY-12465
    Z-Ile-Leu-aldehyde

    Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XII

    Notch γ-secretase Apoptosis Cancer
    Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch.
  • HY-116934
    5-Pentadecylresorcinol

    Adipostatin A

    Others Cancer Infection
    5-Pentadecylresorcinol (Adipostatin A) is a glycerol-3-phosphate dehydrogenase (GPDH) inhibitor with an IC50 of 4.1 µM. Adipostatin A shows good larvicidal activity against Aedes aegypti.
  • HY-115937
    c-Met-IN-9

    c-Met/HGFR Apoptosis Cancer
    c-Met-IN-9, a 4-phenoxypyridine derivative, is a c-Met kinas inhibitor with an IC50 of 12 nM. c-Met-IN-9 induces cells apoptosis, and has antitumor activities.
  • HY-N10332
    Leptosphaerodione

    Proteasome Cancer
    Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC50 value of 3.2 μM. Anti-tumor agent.
  • HY-144448
    FAK-IN-2

    FAK Apoptosis Cancer
    FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
  • HY-15496
    E6201

    ER-806201

    MEK FLT3 Cancer
    E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy.
  • HY-112362
    3-(4-Pyridyl)indole

    Rockout; 3-(4-Pyridinyl)-1H-indole; Rho Kinase inhibitor III, Rockout

    ROCK Inflammation/Immunology
    3-(4-Pyridyl)indole (Rockout) is a Rho-kinase (ROCK) inhibitor, with an IC50 of 25 μM. 3-(4-Pyridyl)indole can inhibit blebbing and cause dissolution of actin stress fibers in a wound healing assay.
  • HY-149019
    Antitumor agent-70

    c-Kit Apoptosis Cancer
    Antitumor agent-70 (compound 8b) has anti-tumor activity and can induce cell apoptosis. Antitumor agent-70 inhibits multiple myeloma with an IC50 value of 0.12 μM. Antitumor agent-70 is a potential multi-targeted kinase inhibitor especially for c-Kit.
  • HY-144870
    STAT3-IN-7

    STAT Cancer
    STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182).
  • HY-149016
    Tubulin polymerization-IN-25

    Microtubule/Tubulin Farnesyl Transferase Cancer
    Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .
  • HY-120696
    SR9186

    ML368

    Cytochrome P450 Parasite Infection
    SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism.
  • HY-113976A
    Endothall

    Endothal

    Phosphatase
    Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy.
  • HY-107550
    HDAC6-IN-7

    HDAC Cancer
    TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells.
  • HY-150505
    DC-U4106

    Deubiquitinase Apoptosis Cancer
    DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer.
  • HY-119425
    Razoxane

    ICRF 159

    Topoisomerase Cancer
    Razoxane (ICRF 159) is an antiangiogenic topoisomerase II inhibitor, can be used for the research of renal cell carcinoma (RCC).
  • HY-145373
    BMS-986143

    Btk Inflammation/Immunology
    BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
  • HY-108585
    VU591 hydrochloride

    Potassium Channel Neurological Disease
    VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM. VU591 hydrochloride can be used for neurological research with HY-108585A (the equivalent of VU591 hydrochloride).
  • HY-108585A
    VU591

    Potassium Channel Neurological Disease
    VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM. VU591 can be used for neurological research with HY-108585 (the equivalent of VU591 hydrochloride).
  • HY-150516S
    BET-IN-12

    Epigenetic Reader Domain Cancer
    BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-145953
    VY-3-135

    Others Cancer
    VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.
  • HY-144102
    HDAC-IN-29

    HDAC Cancer
    HDAC-IN-29 (compound 13b) is a potent pan-HDAC inhibitor. HDAC-IN-29 shows antitumor activity.
  • HY-10580
    GSK 3 Inhibitor IX

    6-Bromoindirubin-3'-oxime; BIO; MLS 2052

    GSK-3 CDK Apoptosis Cancer
    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
  • HY-16929
    Latrunculin A

    LAT-A

    Arp2/3 Complex Cancer
    Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research.
  • HY-147317
    Epothilone E

    Microtubule/Tubulin Cancer
    Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity.
  • HY-150927
    G12Si-2

    Ras Cancer
    G12Si-2, an analog of G12Si-1 (HY-150926), is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12S mutant of K-Ras.
  • HY-142680
    EGFR-IN-23

    EGFR Cancer
    EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8).
  • HY-107613S
    R 59-022-d5

    DKGI-I-d5; Diacylglycerol kinase inhibitor I-d5

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022-d5 (DKGI-I-d5) is the deuterium labeled R 59-022. R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-120290
    PU141

    Histone Acetyltransferase Cancer
    PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
  • HY-121407
    Lateritin

    Acyltransferase Infection Cancer
    Lateritin is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), isolated from the mycelial cake of Gibberella lateritium IFO 7188. Lateritin also inhibits the growth of a mini-panel of human cancer cell lines, gram-positive bacteria, and Candida albicans.
  • HY-144706
    Axl-IN-3

    TAM Receptor Cancer
    Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.
  • HY-117651
    2-Fluoropalmitic acid

    Acyltransferase Cancer
    2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines.
  • HY-117229
    Sonidegib metabolite M48

    Drug Metabolite Cancer
    Sonidegib metabolite M48 is the main circulating metabolite of Sonidegib. Sonidegib is a hedgehog pathway inhibitor. M48 showed a much longer Tmax (60 h) than Sonidegib.
  • HY-143899
    FBA-IN-1

    Fungal Infection
    FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC80 of 1 μg/mL.
  • HY-124805
    MAL3-101

    HSP Cancer
    MAL3-101 is a potent HSP70 allosteric inhibitor. MAL3-101 inhibits HSP70 ATPase activity by blocking Hsp40 co-chaperone interaction. MAL3-101 can be used for researching muscle invasive bladder cancer (MIBC).
  • HY-143483
    NBTIs-IN-5

    Bacterial Infection
    NBTIs-IN-5 (Compound 5r) is a NBTI (Novel Bacterial Topoisomerase Inhibitor) DNA gyrase inhibitor with an IC50 of 1.5 μM against Mycobacterium abscessus (Mabs) DNA gyrase. NBTIs-IN-5 inhibits Mabs bamboo bacterial growth with an MIC90 of 0.4 μM.
  • HY-P9920
    Ramucirumab

    VEGFR Cancer
    Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab is also an angiogenesis inhibitor.
  • HY-10512
    AR-A014418

    AR 0133418; GSK 3β inhibitor VIII; AR 014418

    GSK-3 Metabolic Disease Cancer
    AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM).
  • HY-100950
    ABC1183

    GSK-3 CDK Cancer Inflammation/Immunology
    ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.
  • HY-A0256
    Clavulanic acid

    Antibiotic Bacterial Infection Inflammation/Immunology
    Clavulanic acid is a naturally occurring powerful bacterial β-lactamases inhibitor for research of infections caused by bacteria, including infections of the ears. Clavulanic acid is active against a wide spectrum of gram-positive and gram-negative bacterias.
  • HY-150581
    CYP3A4-IN-3

    Cytochrome P450 Infection Inflammation/Immunology
    CYP3A4-IN-3 is a high-affinity specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.075 μM. CYP3A4-IN-3 is a ritonavir analogue, but with a simpler structure and twice the inhibitory effect of ritonavir. CYP3A4-IN-3 is used as an antiviral agent and immunosuppressant.
  • HY-133747
    JAK3-IN-9

    JAK Inflammation/Immunology
    JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research.
  • HY-B0590
    Tetrabenazine

    Ro 1-9569

    Monoamine Transporter Neurological Disease
    Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
  • HY-B0590E
    Tetrabenazine mesylate

    Ro 1-9569 mesylate

    Monoamine Transporter Neurological Disease
    Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
  • HY-143484
    844-TFM

    Bacterial Infection
    844-TFM is a NBTI (novel bacterial topoisomerase inhibitor) DNA gyrase inhibitor, with an IC50 of 1.5 μM. 844-TFM exhibits bactericidal properties against M. abscessus.
  • HY-N9814
    Shanciol B

    NO Synthase Inflammation/Immunology
    Shanciol B, isolated from the ethyl acetate extract of the air-dried whole plant of Pholidota imbricate Hook, inhibits nitric oxide (NO) production and 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity. Shanciol B is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with anti-inflammatory activity.
  • HY-123346
    SW155246

    DNA Methyltransferase Cancer
    SW155246 is a DNA methyltransferase (DNMT1) selective inhibitor with IC50s of 1.2 and 38 μM for hDNMT1 and mDNMT3A, respectively. SW155246 can be used for the research of cancer and other diseases.
  • HY-108617
    YM976

    Phosphodiesterase (PDE) Inflammation/Immunology
    YM976 is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.2 nM. YM976 shows the dissociation of anti-inflammatory activities from emetic effects and inhibits the antigen-induced airway responses.
  • HY-145389
    SZ-015268

    CDK Cancer
    SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively.
  • HY-150580
    CYP3A4-IN-2

    Cytochrome P450 Cancer Inflammation/Immunology
    CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.055 μM. CYP3A4-IN-2 is a ritonavir analogue with increased hydrophobicity of the R2 side group and stronger inhibitory effect compared to ritonavir. CYP3A4-IN-2 can be used as an antiviral agent and immunosuppressants.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-N10472
    STAT3-IN-14

    STAT Cancer
    STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3.
  • HY-146275
    LXRβ agonist-3

    LXR Cancer
    LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma.
  • HY-147960
    Glycosyltransferase-IN-1

    Bacterial Infection
    Glycosyltransferase-IN-1 (compound 5m) is a potent glycosyltransferase inhibitor, with an IC50 of 82.8 μM. Glycosyltransferase-IN-1 shows antibacterial activity, with MIC values of 6 μg/mL for MSSA, MRSA, B. subtilis and 12 μg/mL for E. coli.
  • HY-145594
    Safusidenib

    Isocitrate Dehydrogenase (IDH) Cancer
    Safusidenib is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
  • HY-D0961
    Gallocyanine chloride

    Wnt Neurological Disease
    Gallocyanine chloride, a synthetic blue dyestuff, blocks DKK1 inhibitory activity by disrupting DKK1/LRP6 interaction. Its association with LRP6 is weak (IC50 of about 3 μM in the inhibition of DKK1 binding). Gallocyanine dye acts as a potential agent for the research of Alzheimer's disease and related neurodegenerative tauopathies.
  • HY-151351
    SphK2-IN-2

    SphK Cancer
    SphK2-IN-2 (21g) is a potent and selective SphK2 inhibitor with an IC50 value of 0.23 μM.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-15445
    CTEP

    RO 4956371; mGluR5 inhibitor

    mGluR Neurological Disease
    CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
  • HY-147243
    Ansornitinib

    ANG-3070

    VEGFR PDGFR Inflammation/Immunology Cardiovascular Disease
    Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-150685
    Topo I/COX-2-IN-1

    Topoisomerase Prostaglandin Receptor Apoptosis Cancer Inflammation/Immunology
    Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity.
  • HY-145588A
    Povorcitinib phosphate

    JAK Inflammation/Immunology
    Povorcitinib phosphate is a potent and selective inhibitor of JAK1. Povorcitinib phosphate has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP).
  • HY-147694
    c-Met-IN-11

    c-Met/HGFR VEGFR Cancer
    c-Met-IN-11 (compound 3) is a potent c-MET and VEGFR-2 inhibitor, with IC50 values of 41.4 and 71.1 nM, respectively.
  • HY-121725
    MM-206

    STAT Cancer
    MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines.
  • HY-145155
    Calpain-2-IN-1

    Proteasome Neurological Disease
    Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function.
  • HY-150967
    MmpL3-IN-1

    Bacterial Infection
    MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis.
  • HY-144813
    Gü2602

    Cathepsin Cancer Inflammation/Immunology
    Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
  • HY-19348
    Pimelic Diphenylamide 106

    RGFA-8; TC-H 106; Histone Deacetylase inhibitor VII

    HDAC Cancer
    Pimelic Diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.
  • HY-147851
    BACE1-IN-12

    Beta-secretase Neurological Disease
    BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent.
  • HY-150728
    AChE-IN-22

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease.
  • HY-147746
    MMP2-IN-3

    MMP Cancer
    MMP2-IN-3 (compound 2) is a potent MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 31 μM. MMP2-IN-3 also shows inhibitory activity against MMP-9 and MMP-8, with IC50 values of 26.6, and 32 μM, respectively.
  • HY-144812
    Gü1303

    Cathepsin Cancer Inflammation/Immunology
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
  • HY-106011
    SLX-4090

    Others Metabolic Disease
    SLX-4090 is an orally active enterocytic-specific microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 8.0 nM. SLX-4090 can be used for the research of dyslipidemia.
  • HY-146958
    MAO-B-IN-8

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-8 is a potent reversible MAO-B inhibitor and an inhibitor of microglial production of neuroinflammatory mediator. MAO-B-IN-8 can be used for neurodegenerative disease research.
  • HY-147922
    hCAI/II-IN-2

    Carbonic Anhydrase Inflammation/Immunology
    hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
  • HY-147923
    hCAI/II-IN-3

    Carbonic Anhydrase Inflammation/Immunology
    hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
  • HY-146128
    Anti-hyperglycemic agent-1

    Glucosidase Metabolic Disease
    Anti-hyperglycemic agent-1 (compound 10) is a potent α-Glucosidase inhibitor, with an IC50 of 0.53 μM. Anti-hyperglycemic agent-1 can be used for diabetes research.
  • HY-119390
    AA-CW236

    DNA Methyltransferase Cancer
    AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification.
  • HY-B0118A
    Vecuronium bromide

    ORG NC 45

    nAChR Cancer Neurological Disease
    Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia.
  • HY-117724
    AZ3976

    PAI-1 Cardiovascular Disease
    AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-147745
    MMP2-IN-2

    MMP Cancer
    MMP2-IN-2 (compound 42) is a potent and selective MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 4.2 μM. MMP2-IN-2 also shows inhibitory activity against MMP-13, MMP-9 and MMP-8, with IC50 values of 12, 23.3, and 25 μM, respectively.
  • HY-132993
    Hcyb1

    Phosphodiesterase (PDE) Neurological Disease
    Hcyb1 is a highly selective, orally active PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling.
  • HY-143873
    Bcl-2-IN-5

    Bcl-2 Family Cancer
    Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155).
  • HY-150041
    TL4830031

    TAM Receptor Cancer
    TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.
  • HY-150566
    BCR-ABL-IN-5

    Bcr-Abl Cancer
    BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells.
  • HY-150550
    COX-2-IN-26

    COX Inflammation/Immunology
    COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile.
  • HY-117374
    HDAC3-IN-1

    HDAC Cancer
    HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM.
  • HY-146108
    RSV-IN-5

    RSV Infection
    RSV-IN-5 (Compound 4) is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. RSV-IN-5 exhibits potent anti-RSV activities against not only wild-type A2 F protein (EC50=2.0 nM), but also D486N-mutant F protein (EC50=8.1 nM).
  • HY-124063
    BI-1935

    Epoxide Hydrolase Cardiovascular Disease
    BI-1935 is a potent soluble epoxide hydrolase (sEH) inhibitor. BI-1935 can be used for the research of cardiovascular disease.
  • HY-144820
    JO146

    Ser/Thr Protease Infection
    JO146 is a Chlamydia trachomatis high temperature requirement A (CtHtrA) protease inhibitor with IC50s of 21.86 and 1.15 μM for CtHtrA and human neutrophil elastase (HNE), respectively. JO146 can be used to inhibits bacterial infections.
  • HY-144270
    Glucosylceramide synthase-IN-3

    Others Metabolic Disease Neurological Disease
    Glucosylceramide synthase-IN-3 (compound BZ1) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 16 nM for human GCS.Glucosylceramide synthase-IN-3 can be used for Gaucher's disease research.
  • HY-150761
    MY-875

    Microtubule/Tubulin Apoptosis Cancer
    MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity.
  • HY-115928
    M24

    Bcl-2 Family Cancer
    M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells.
  • HY-113492
    5(S)15(S)-DiHETE

    Interleukin Related Inflammation/Immunology Cardiovascular Disease
    5(S)15(S)-DiHETE is an “activated” intermediate, inhibits platelet aggregation with an IC50 of 1.3 μM. 5(S)15(S)-DiHETE enhances the rate of either LXA4 or LXB4 biosynthesis.
  • HY-B0466A
    Cloxacillin

    Antibiotic Bacterial Cancer Infection Inflammation/Immunology
    Cloxacillin is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.
  • HY-B0466
    Cloxacillin sodium monohydrate

    Bacterial Antibiotic Infection Inflammation/Immunology Cancer
    Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium monohydrate can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.
  • HY-B0466B
    Cloxacillin sodium

    Bacterial Antibiotic Infection Inflammation/Immunology Cancer
    Cloxacillin sodium is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.
  • HY-147967
    EGFR-IN-63

    EGFR Cancer
    EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-142517
    EGFR-IN-25

    EGFR Cancer
    EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively.
  • HY-144266
    Glucosylceramide synthase-IN-1

    Others Metabolic Disease Neurological Disease
    Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research.
  • HY-151211
    BTK-IN-16

    Btk Cancer Inflammation/Immunology
    BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia.
  • HY-131976
    BVDV-IN-1

    DNA/RNA Synthesis Infection
    BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. BVDV-IN-1 directly binds to a hydrophobic pocket of the BVDV RdRp. BVDV-IN-1 has antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC).
  • HY-N7661
    4β-Hydroxywithanolide E

    PPAR Metabolic Disease
    4β-Hydroxywithanolide E, isolated from Physalis peruviana L., inhibits adipocyte differentiation of 3T3-L1 cells through modulation of mitotic clonal expansion. 4β-Hydroxywithanolide E is an adipogenesis inhibitor and inhibits PPARγ, C/EBPα, and the adipocyte-specific molecule aP2 mRNA expression.
  • HY-121093
    DC-S239

    Histone Methyltransferase Cancer
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity.
  • HY-15899
    Des(benzylpyridyl) Atazanavir

    HIV Protease HIV Drug Metabolite Infection
    Des(benzylpyridyl) Atazanavir (compound M1) is a N-dealkylation product of Atazanavir (HY-17367) metabolite. Atazanavir is a highly selective HIV-1 protease inhibitor. Des(benzylpyridyl) Atazanavir may contribute to the effectiveness Atazanavir but also to the toxicity and interactions. Des(benzylpyridyl) Atazanavir can be used for further research of Atazanavir effects.
  • HY-115902
    FGFR4-IN-7

    FGFR Apoptosis Cancer
    FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC).
  • HY-132246
    WWL123

    MAGL Neurological Disease
    WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice.
  • HY-144689
    BChE-IN-3

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE.
  • HY-144188
    PRMT5-IN-17

    Histone Methyltransferase Cancer
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
  • HY-144187
    PRMT5-IN-16

    Histone Methyltransferase Cancer
    PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
  • HY-10515
    BX-320

    PDK-1 Cancer
    BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.
  • HY-A0115
    Ramiprilat

    HOE 498 diacid; Ramipril diacid

    Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research.
  • HY-144612
    NS2B/NS3-IN-2

    Virus Protease Infection
    NS2B/NS3-IN-2 is a potent dengue virus (DENV) NS2B/NS3 covalent inhibitor with an IC50 of 6.0 nM and Ki of 0.66 µM. NS2B/NS3-IN-2 shows no cytotoxicity and markedly increases the cell survival rate.
  • HY-124346
    T-3364366

    Others Metabolic Disease
    T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay.
  • HY-108647
    EO 1428

    p38 MAPK Inflammation/Immunology
    EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.
  • HY-149030
    DHODH-IN-21

    Dihydroorotate Dehydrogenase Cancer
    DHODH-IN-21 (compound 19) is an orally active selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 1.1 nM. DHODH-IN-21 has anticancer activity and can be used in studies of acute myeloid leukaemia (AML).
  • HY-124379
    TPCK

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    Ser/Thr Protease HPV Cancer Inflammation/Immunology
    TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium.
  • HY-139690
    CCG258747

    Opioid Receptor Cardiovascular Disease
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
  • HY-150587
    Anti-inflammatory agent 31

    ERK NF-κB Inflammation/Immunology
    Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver.
  • HY-115974
    GRPR antagonist-1

    Others Cancer
    GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.
  • HY-145303
    DX2-201

    Mitochondrial Metabolism Cancer
    DX2-201 is a potent and selective oxidative phosphorylation (OXPHOS) complex I inhibitor with an IC50 of 312 nM. DX2-201 has anticancer effects.
  • HY-B0307A
    Idoxuridine hydrate

    5-Iodo-2′-deoxyuridine hydrate; 5-IUdR hydrate; IdUrd hydrate

    Phosphatase Infection
    Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) hydrate is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM.
  • HY-150699
    TXA6101

    Bacterial Infection
    TXA6101 is a bacterial protein FtsZ (filamentous temperature-sensitive protein Z) inhibitor that inhibits bacterial division. TXA6101 has antimicrobial activity against MRSA isolates expressing either the G193D or G196S mutant FtsZ with the MIC value of 1 μg/mL, retains significant activity against the TXA707-resistant FtsZ mutant. TXA6101 can be used as a potential method against Gram-negative bacterial infections.